Cyclic_somatostatin_DataSheet_MedChemExpress

SMILES：O=C(OC1=CC=CC([C@@H](N(C)C)C)=C1)N(CC)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O
参考文献：
[1]. Kurz A, Farlow M, Lefèvre G. Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review. Int J Clin Pract. 2009 May;63(5):799-805.
中文别名：
酒石酸卡巴拉汀;(S)-N-乙基-N-甲基氨基甲酸-3-[(1-二甲氨基)乙基]苯酯酒石酸盐;卡巴拉汀或利斯的明酒石酸盐;L-酒石酸卡巴拉汀;2,3',4-三溴二苯醚;N-乙基甲基氨基甲酰氯;Rivastigmine L-Tartrate L-酒石酸卡巴拉汀;酒石酸卡巴拉汀 USP标准品;酒石酸卡巴拉汀Rivastigmine tartrate;酒石酸卡巴拉汀标准品;酒石酸卡巴拉汀氢 EP标准品;酒石酸利凡斯的明;卡巴拉丁;卡巴拉汀酒石酸盐;重酒石酸卡巴拉汀;重酒石酸利凡斯的明;(S)-N-乙基-N-甲基氨基甲酸-3-[(S)-1-(二甲氨基)乙基]苯酯酒石酸盐;氘代重酒石酸利斯的明-d6;酒石酸卡巴拉汀 中文别名：卡巴拉汀或利斯的明酒石酸盐;酒石酸利伐斯的明;酒石酸利瓦斯汀;利斯的明酒石酸盐;卡巴拉汀重酒石酸盐
熔点
123-1250C
分子式
C18H28N2O8
分子量
400.423
闪点
145ºC
精确量
400.18457
PSA
147.84
LogP
0.6371

过氧化物酶体增殖物激活受体(PPAR) 是一类由配体激活的核转录因子,属Ⅱ型核受体超家族成员, 存在3种亚型，即PPARα、PPARδ、PPARγ，这三种亚型在结构上有一定的相似性，均含DNA结合区和配体结合区等。

PPAR与配体结合后被激活，与9-顺视黄酸类受体形成异二聚体，然后与靶基因的启动子上游的过氧化物酶体增殖物反应元件(peroxisome proliferator response element，PPRE)结合而发挥转录调控作用。

PPRE 由含相隔一个或两个核苷酸的重复序列AGGTCA组成。

与配体结合后，PPAR在DNA结合区发生变构，进而影响PPAR刺激靶基因转录的能力。

PPARδ几乎在所有组织中表达，浓度低于PPARα及PPARγ，直至最近以前尚未找到此一核受体的选择性配基。

PPARδ是代谢综合征（肥胖、胰岛素抵抗、高血压是与脂质紊乱有关的共同的病态表现）的一个新靶点。

有不少的研究表明：GW501516可作为PPARδ的特异激动剂用于研究。

参考网址：/cjh/2003/shownews.asp?id=156/conference/preview.php?kind_id=03&cat_name=ADA2001&title_id=59219 Regulation of Muscle Fiber Type and Running Endurance by PPARδplos biology，Volume 2 | Issue 10 | October 2004/plosonline/?request=get-document&doi=10.1371%2Fjournal.pbio.0020294NF-KB通路中的抑制剂好像有1.PDTC(pyrrolidine dithiocarbamate),是一种抗氧化剂，主要作用于IκB降解的上游环节（IκBα的磷酸化或IKK的活性水平），2.Gliotoxin 是一种免疫抑制剂，机制可能从多个环节阻断NF-KB的激活，如IκB的降解，NF-KB的核移位和与DNA的结合。

Calculate the quantity, in mg, of thiamine hydrochloride (C12H17ClN4OS·HCl) in the assay material on the basis of the ali-quots taken. Where indicated, the quantity, in mg, of thiamine mononitrate (C12H17N5O4S) may be calculated by multiplyingthe quantity of C12H17ClN4OS·HCl found by 0.9706.á541ñ TITRIMETRYDirect Titrations—Direct titration is the treatment of a soluble substance, contained in solution in a suitable vessel (the titrate), with an appropriate standardized solution (the titrant), the endpoint being determined instrumentally or visually with the aid of a suitable indicator.The titrant is added from a suitable buret and is so chosen, with respect to its strength (normality), that the volume added is between 30% and 100% of the rated capacity of the buret. [N OTE—Where less than 10 mL of titrant is required, a suitable microburet is to be used.] The endpoint is approached directly but cautiously, and finally the titrant is added dropwise from the buret in order that the final drop added will not overrun the endpoint. The quantity of the substance being titrated may be calculated from the volume and the normality or molarity factor of the titrant and the equivalence factor for the substance given in the individual monograph.Residual Titrations—Some Pharmacopeial assays require the addition of a measured volume of a volumetric solution, in excess of the amount actually needed to react with the substance being assayed, the excess of this solution then being titrated with a second volumetric solution. This constitutes a residual titration and is known also as a “back titration.” The quantity of the substance being titrated may be calculated from the difference between the volume of the volumetric solution originally added, corrected by means of a blank titration, and that consumed by the titrant in the back titration, due allowance being made for the respective normality or molarity factors of the two solutions, and the equivalence factor for the substance given in the individual monograph.Complexometric Titrations—Successful complexometric titrations depend on several factors. The equilibrium constant for formation of the titrant-analyte complex must be sufficiently large that, at the endpoint, very close to 100% of the analyte has been complexed. The final complex must be formed rapidly enough that the analysis time is practical. When the analytical reaction is not rapid, a residual titration may sometimes be successful.In general, complexometric indicators are themselves complexing agents. The reaction between metal ion and indicator must be rapid and reversible. The equilibrium constant for formation of the metal-indicator complex should be large enough to produce a sharp color change but must be less than that for the metal-titrant complex. Indicator choice is also restricted by the pH range within which the complexation reaction must be carried out and by interference of other ions arising from the sample or the buffer. Interfering ions may often be masked or “screened” via addition of another complexing agent. (The masking technique is also applicable to redox titrations.)Oxidation-Reduction (Redox) Titrations—Determinations may often be carried out conveniently by the use of a reagent that brings about oxidation or reduction of the analyte. Many redox titration curves are not symmetric about the equivalence point, and thus graphical determination of the endpoint is not possible; but indicators are available for many determinations, and a redox reagent can often serve as its own indicator. As in any type of titration, the ideal indicator changes color at an endpoint that is as close as possible to the equivalence point. Accordingly, when the titrant serves as its own indicator, the difference between the endpoint and the equivalence point is determined only by the analyst's ability to detect the color change. A common example is the use of permanganate ion as an oxidizing titrant since a slight excess can easily be detected by its pink color. Other titrants that may serve as their own indicators are iodine, cerium (IV) salts, and potassium dichromate. In most cases, however, the use of an appropriate redox indicator will yield a much sharper endpoint.It may be necessary to adjust the oxidation state of the analyte prior to titration through use of an appropriate oxidizing or reducing agent; the excess reagent must then be removed, e.g., through precipitation. This is nearly always the practice in the determination of oxidizing agents since most volumetric solutions of reducing agents are slowly oxidized by atmospheric oxy-gen.Titrations in Nonaqueous Solvents—Acids and bases have long been defined as substances that furnish, when dissolved in water, hydrogen and hydroxyl ions, respectively. This definition, introduced by Arrhenius, fails to recognize the fact that prop-erties characteristic of acids or bases may be developed also in other solvents. A more generalized definition is that of Bröns-ted, who defined an acid as a substance that furnishes protons, and a base as a substance that combines with protons. Even broader is the definition of Lewis, who defined an acid as any material that will accept an electron pair, a base as any material that will donate an electron pair, and neutralization as the formation of a coordination bond between an acid and a base.The apparent strength of an acid or a base is determined by the extent of its reaction with a solvent. In water solution all strong acids appear equally strong because they react with the solvent to undergo almost complete conversion to oxonium ion and the acid anion (leveling effect). In a weakly protophilic solvent such as acetic acid the extent of formation of the ace-tate acidium ion shows that the order of decreasing strength for acids is perchloric, hydrobromic, sulfuric, hydrochloric, andnitric (differentiating effect).Acetic acid reacts incompletely with water to form oxonium ion and is, therefore, a weak acid. In contrast, it dissolves in a base such as ethylenediamine, and reacts so completely with the solvent that it behaves as a strong acid. The same holds for perchloric acid.This leveling effect is observed also for bases. In sulfuric acid almost all bases appear to be of the same strength. As the acid properties of the solvent decrease in the series sulfuric acid, acetic acid, phenol, water, pyridine, and butylamine, the bases become progressively weaker until all but the strongest have lost their basic properties. In order of decreasing strength, the strong bases are sodium 2-aminoethoxide, potassium methoxide, sodium methoxide, and lithium methoxide.Many water-insoluble compounds acquire enhanced acidic or basic properties when dissolved in organic solvents. Thus the choice of the appropriate solvent permits the determination of a variety of such materials by nonaqueous titration. Further-more, depending upon which part of a compound is the physiologically active moiety, it is often possible to titrate that part by proper selection of solvent and titrant. Pure compounds can be titrated directly, but it is often necessary to isolate the active ingredient in pharmaceutical preparations from interfering excipients and carriers.The types of compounds that may be titrated as acids include acid halides, acid anhydrides, carboxylic acids, amino acids,enols such as barbiturates and xanthines, imides, phenols, pyrroles, and sulfonamides. The types of compounds that may be titrated as bases include amines, nitrogen-containing heterocyclic compounds, oxazolines, quaternary ammonium com-pounds, alkali salts of organic acids, alkali salts of weak inorganic acids, and some salts of amines. Many salts of halogen acids may be titrated in acetic acid or acetic anhydride after the addition of mercuric acetate, which removes halide ion as the unionized mercuric halide complex and introduces the acetate ion.For the titration of a basic compound, a volumetric solution of perchloric acid in glacial acetic acid is preferred, although perchloric acid in dioxane is used in special cases. The calomel-glass electrode system is useful in this case. In acetic acid sol-vent, this electrode system functions as predicted by theory.For the titration of an acidic compound, two classes of titrant are available: the alkali metal alkoxides and the tetraalkylam-monium hydroxides. A volumetric solution of sodium methoxide in a mixture of methanol and toluene is used frequently, al-though lithium methoxide in methanol-benzene solvent is used for those compounds yielding a gelatinous precipitate on titra-tion with sodium methoxide.The alkali error limits the use of the glass electrode as an indicating electrode in conjunction with alkali metal alkoxide ti-trants, particularly in basic solvents. Thus, the antimony-indicating electrode, though somewhat erratic, is used in such titra-tions. The use of quaternary ammonium hydroxide compounds, e.g., tetra-n -butylammonium hydroxide and trimethylhexade-cylammonium hydroxide (in benzene-methanol or isopropyl alcohol), has two advantages over the other titrants in that (a)the tetraalkylammonium salt of the titrated acid is soluble in the titration medium, and (b) the convenient and well-behaved calomel-glass electrode pair may be used to conduct potentiometric titrations.Because of interference by carbon dioxide, solvents for acidic compounds need to be protected from excessive exposure to the atmosphere by a suitable cover or by an inert atmosphere during the titration. Absorption of carbon dioxide may be deter-mined by performing a blank titration. The blank should not exceed 0.01 mL of 0.1 N sodium methoxide VS per mL of sol-vent.The endpoint may be determined visually by color change, or potentiometrically, as indicated in the individual monograph.If the calomel reference electrode is used, it is advantageous to replace the aqueous potassium chloride salt bridge with 0.1 N lithium perchlorate in glacial acetic acid for titrations in acidic solvents or potassium chloride in methanol for titrations in basic solvents.Where these or other mixtures are specified in individual monographs, the calomel reference electrode is modified by first removing the aqueous potassium chloride solution and residual potassium chloride, if any, by rinsing with water, then elimi-nating residual water by rinsing with the required nonaqueous solvent, and finally filling the electrode with the designated nonaqueous mixture.In nearly all cases, except those where silver ion might interfere, a silver-silver chloride reference electrode may be substitu-ted for the calomel electrode. The silver-silver chloride electrode is more rugged, and its use helps to eliminate toxic mercury salts from the laboratory. Generally, a salt bridge may be used to circumvent interference by silver ion.The more useful systems for titration in nonaqueous solvents are listed in Table 1.Table 1. Systems for Nonaqueous TitrationsType ofAcidic (for titrationof bases and theirsalts)Relatively Neutral(for differentialtitration of bases)Basic (for titrationof acids)Relatively Neutral(for differentialtitration of acids) Solvent1Glacial Acetic Acid Acetonitrile Dimethylformamide AcetoneAcetic Anhydride Alcohols n-Butylamine AcetonitrileFormic Acid Chloroform Pyridine Methyl Ethyl KetonePropionic Acid Benzene Ethylenediamine Methyl Isobutyl KetoneSulfuryl Chloride Toluene Morpholine tert-Butyl AlcoholChlorobenzeneEthyl AcetateDioxaneIndicator Crystal Violet Methyl Red Thymol Blue Azo VioletQuinaldine Red Methyl Orange Thymolphthalein Bromothylmol Bluep-Naphtholbenzein p-Naphtholbenzein Azo Violet p-HydroxyazobenzeneAlphezurine 2-G o-Nitroaniline Thymol BlueMalachite Green p-HydroxyazobenzeneElectrodes Glass–calomel Glass–calomel Antimony–calomel Antimony–calomelGlass–silver–silver chloride Calomel–silver–silverchlorideAntimony–glass Glass–calomelMercury–mercuric acetate Antimony–antimony2Glass–platinum2Platinum–calomelGlass–calomel1 Relatively neutral solvents of low dielectric constant such as benzene, toluene, chloroform, or dioxane may be used in conjunction with any acidic or basic solvent in order to increase the sensitivity of the titration end-points.2 In titrant.Indicator and Potentiometric Endpoint Detection—The simplest and most convenient method by which the equivalence point, i.e., the point at which the stoichiometric analytical reaction is complete, may be determined is with the use of indica-tors. These chemical substances, usually colored, respond to changes in solution conditions before and after the equivalence point by exhibiting color changes that may be taken visually as the endpoint, a reliable estimate of the equivalence point.A useful method of endpoint determination results from the use of electrochemical measurements. If an indicator electrode, sensitive to the concentration of the species undergoing titrimetric reaction, and a reference electrode, whose potential is in-sensitive to any dissolved species, are immersed in the titrate to form a galvanic cell, the potential difference between the elec-trodes may be sensed by a pH meter and used to follow the course of the reaction. Where such a series of measurements is plotted correctly (i.e., for an acid-base titration, pH versus mL of titrant added; for a precipitimetric, complexometric, or oxida-tion-reduction titration, mV versus mL of titrant added), a sigmoid curve results with a rapidly changing portion (the “break”) in the vicinity of the equivalence point. The midpoint of this linear vertical portion or the inflection point may be taken as the endpoint. The equivalence point may also be determined mathematically without plotting a curve. However, it should be no-ted that in asymmetrical reactions, which are reactions in which the number of anions reacting is not the same as the number of cations reacting, the endpoint as defined by the inflection of the titration curve does not occur exactly at the stoichiometric equivalence point. Thus, potentiometric endpoint detection by this method is not suitable in the case of asymmetric reactions, examples of which are the precipitation reaction,2Ag+ + CrO4–2and the oxidation-reduction reaction,5Fe+2 + MnO4–.All acid-base reactions, however, are symmetrical. Thus, potentiometric endpoint detection may be employed in acid-base ti-trations and in other titrations involving symmetrical reversible reactions where an indicator is specified, unless otherwise direc-ted in the individual monograph.Two types of automatic electrometric titrators are available. The first is one that carries out titrant addition automatically and records the electrode potential differences during the course of titration as the expected sigmoid curve. In the second type, titrant addition is performed automatically until a preset potential or pH, representing the endpoint, is reached, at which point the titrant addition ceases.Several acceptable electrode systems for potentiometric titrations are summarized in Table 2.Table 2. Potentiometric Titration Electrode SystemsTitration Indicating Electrode Equation 1Reference Electrode Applicability 2Acid-base Glass E = k + 0.0591 pH Calomel or silver–silver chlorideTitration of acids and basesPrecipitimetric (silver)Silver E = E° + 0.0591 log [Ag +]Calomel (with potassium ni-trate salt bridge)Titration with or of silver in-volving halides or thiocya-nateComplexometric Mercury–mercury(II) E = E° + 0.0296(log k ¢ − pM)Calomel Titration of various metals(M), e.g., Mg +2, Ca +2 Al +3,Bi +3, with EDTAOxidation–reduction Platinum E = E° + (0.0591/n) × log [ox]/[red]Calomel or silver–silver chloride Titrations with arsenite, bro-mine, cerate, dichromate,exacyonoferrate(III), iodate,nitrite, permanganate, thio-sulfate1 Appropriate form of Nernst equation describing the indicating electrode system: k = glass electrode constant; k ¢ = constant derived from Hg–Hg(II)–EDTA equi-librium; M = any metal undergoing EDTA titration; [ox] and [red] from the equation, ox + n e ®¬red.2Listing is representative but not exhaustive.Blank Corrections—As previously noted, the endpoint determined in a titrimetric assay is an estimate of the reaction equiv-alence point. The validity of this estimate depends upon, among other factors, the nature of the titrate constituents and theconcentration of the titrant. An appropriate blank correction is employed in titrimetric assays to enhance the reliability of theendpoint determination. Such a blank correction is usually obtained by means of a residual blank titration , wherein the required procedure is repeated in every detail except that the substance being assayed is omitted. In such instances, the actual volumeof titrant equivalent to the substance being assayed is the difference between the volume consumed in the residual blank titra-tion and that consumed in the titration with the substance present. The corrected volume so obtained is used in calculatingthe quantity of the substance being titrated, in the same manner as prescribed under Residual Titrations . Where potentiometricendpoint detection is employed, the blank correction is usually negligible.á551ñ VITAMIN E ASSAYINTRODUCTIONThe following liquid chromatographic procedures are provided for the determination of vitamin E as an active pharmaceutical ingredient, as a dietary supplement ingredient, or as a component in compendial dosage forms in the forms of alpha toco-pherol (C 29H 50O 2), alpha tocopheryl acetate (C 31H 52O 3), or alpha tocopheryl acid succinate (C 33H 54O5).Throughout this assay, protect solutions containing, and derived from, the test specimen and the Reference Standard from the atmosphere and light, preferably by the use of a blanket of inert gas and low-actinic glassware.Where vitamin E (alpha tocopherol, alpha tocopheryl acetate, or alpha tocopheryl acid succinate) is specified in the following procedure, use the chemical form present in the formulation and the relevant USP Reference Standard.ASSAY• P ROCEDURE 1•This procedure can be used to determine vitamin E in:•Oil-Soluble Vitamins Tablets•Oil-Soluble Vitamins Capsules•Oil-Soluble Vitamins with Minerals Tablets•Oil-Soluble Vitamins with Minerals Capsules•Oil- and Water-Soluble Vitamins Tablets•Oil- and Water-Soluble Vitamins Capsules•Oil- and Water-Soluble Vitamins with Minerals Tablets•Oil- and Water-Soluble Vitamins with Minerals Capsules•This is a neutral procedure that involves the use of dimethyl sulfoxide to dissolve the excipients in the sample, fol-lowed by a liquid–liquid extraction of vitamin E with hexane. The hexane extract is then evaporated in vacuum todryness, and the residue is reconstituted in methanol prior injection into the chromatograph.•Unless specified in the individual monographs, the System suitability solution , Standard solution , Sample solutions , and reagent solutions are prepared as follows.Solution A:Phosphoric acid solution (1 in 100) in waterMobile phase: Methanol and Solution A (19:1)。

IT1t dihydrochloride
1092776-63-0
10mg
≥98%
品牌
货号
中文名称
英文名称
CAS
包装
纯度
MedBio
MED13391
MF498
MF498
915191-42-3
5mg
≥98%
品牌
货号
中文名称
英文名称
CAS
包装
纯度
MedBio
MED12993
Rauwolscine hydrochloride
【脉铂小课堂】MedBio生长抑素受体拮抗剂
1、Cyclosomatostatin物理参数：
常用名
Cyclosomatostatin
英文名
Cyclosomatostatin
CAS号
84211-54-1
分子量
779.96700
密度
1.147g/cm3
沸点
1118.4ºC at 760 mmHg
分子式
C44H57N7O6
英文名称
CAS
包装
纯度
MedBio
MED12706
CGRP 8-37 (human)
CGRP 8-37 (human)
119911-68-1
5mg
≥98%
品牌
货号
中文名称
英文名称
CAS
包装
纯度
MedBio
MED12892
YE 120
YE 120
383124-82-1
50mg
≥98%
品牌
货号
中文名称
英文名称
≥98%
品牌
货号
中文名称