R-IMPP_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:YM–58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca 2+ signals.In Vitro: YM–58483 can decrease the levels of P–ERK and P–CREB, without affecting the expression of CD11b andGFAP. YM–58483 also inhibits the release of spinal cord IL–1β, TNF–α, and PGE2[1]. YM–58483 and cyclosporine A inhibits T cell proliferation in a one–way mixed lymphocyte reaction (mLR) with IC 50 values of 330 and 12.7 nM, respectively [2]. YM–58483 inhibits DNP antigen–induced histamine release from and leukotrienes (LTs) production in IgE–primed RBL–2H3 cells, a rat basophilic leukemia cell line, with IC 50 values of 460 and 310 nM, respectively. YM–58483 also inhibits phytohemagglutinin–P (PHA)–stimulated IL–5 and IL–13 production in human peripheral blood cells with IC 50 values of 125 and 148 nM, respectively, which is approximately 5 times less potent than prednisolone [3]. YM–58483 inhibits IL–4 and IL–5 production in a conalbumine–stimulated murine Th2 T cellclone (D10.G4.1), and IL–5 production in phytohemagglutinin–stimulated human whole blood cells with IC 50 values comparable to those reported for its CRAC channel inhibition (around 100 nM)[4].In Vivo: Intrathecal YM–58483 at the concentration of 300 μM (1.5 nmol) and 1000 μM (10 nmol) produces a significant central analgesic effect on the SNL rats [1]. In the mouse graft–versus–host disease (GVHD) model, YM–58483 (1–30 mg/kg, p.o.) and cyclosporine A (1–30 mg/kg, p.o.) inhibit donor anti–host cytotoxic T lymphocyte (CTL) activity and IFN–γ production, and also reduce the number of donor T cells, especially donor CD8+ T cells, in the spleen. YM–58483 (1–10 mg/kg, p.o.) and cyclosporine A (2, 10 mg/kg, p.o.) inhibit the sheep red blood cell (SRBC)–induced delayed type hypersensitivity (DTH) response [2]. M–58483 (30mg/kg, p.o.) significantly suppresses ovalbumin (OVA)–induced bronchoconstriction in OVA–sensitized guinea pigs, whereas prednisolone does not. YM–58483 (3–30 mg/kg, p.o.) and prednisolone (100 mg/kg, p.o.) both significantly and completelysuppress airway hyperresponsiveness (AHR) caused by OVA exposure [3]. YM–58483 inhibits antigen–induced eosinophil infiltration into airways, and decreases IL–4 and cysteinyl–leukotrienes content in inflammatory airways induced in actively sensitized Brown Norway rats. Orally administered YM–58483 prevents antigen–induced late phase asthmatic broncoconstriction and eosinophil infiltration in actively sensitized guinea pigs [4].PROTOCOL (Extracted from published papers and Only for reference)Animal Administration: YM–58483 is suspended in 0.5% methylcellulose solution for oral administration at a volume of 10mL/kg.[2]Male Balb/c mice are immunized by subcutaneous injection of SRBC (2×107 cells) on day 0. Immunized mice are challenged with 30 μL of 1×108 SRBC into the left hind footpad on day 5. Footpad swelling is measured 24 h after the challenge using a thickness gauge and expressed as the difference between the thickness of the left footpad and that of the right one, which receives an equal volume of 0.9% saline. As a negative control, male Balb/c mice are injected with 0.9% saline and challenged with SRBC. YM–58483 and cyclosporine A are administered orally once daily from day 0 to day 5 (6 consecutive days).Product Name:YM–58483Cat. No.:HY-100831CAS No.:223499-30-7Molecular Formula:C 15H 9F 6N 5OS Molecular Weight:421.32Target:CRAC Channel Pathway:Membrane Transporter/Ion Channel Solubility:DMSO: ≥ 32 mg/mLReferences:[1]. Qi Z, et al. The Central Analgesic Mechanism of YM–58483 in Attenuating Neuropathic Pain in Rats. Cell Mol Neurobiol. 2016 Oct;36(7):1035–43.[2]. Ohga K, et al. Characterization of YM–58483/BTP2, a novel store–operated Ca2+ entry blocker, on T cell–mediated immune responses in vivo. Int Immunopharmacol. 2008 Dec 20;8(13–14):1787–92[3]. Ohga K, et al. The suppressive effects of YM–58483/BTP–2, a store–operated Ca2+ entry blocker, on inflammatory mediator release in vitro and airway responses in vivo. Pulm Pharmacol Ther. 2008;21(2):360–9.[4]. Yoshino T, et al. YM–58483, a selective CRAC channel inhibitor, prevents antigen–induced airway eosinophilia and late phase asthmatic responses via Th2 cytokine inhibition in animal models. Eur J Pharmacol. 2007 Apr 10;560(2–3):225–33.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

References: [1]. Kang J, et al. Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005 Mar;67(3):827-36.
Caution: Not fully tested. For research purposes only Medchemexpress LLC

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Product Data Sheet
RPR-260243 668463-35-2 HY-16915 510.50 C28H25F3N2O4 >98%
Product Name: CAS No.: Cat. No.: MWt: Formula: Purity O: 46mg/mL
Mechanisms: Pathways:Membrane Tranporter/Ion Channel; Target:Potassium Channel Biological Activity: RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes. IC50 value: Target: HERG activator RPR260243 displayed no activator-like effects on other voltage-dependent ion channels, including the closely related erg3 K+ channel. RPR260243 enhanced the delayed rectifier current in guinea pig myocytes but, when administered alone, had little effect on action potential parameters in these cells. However, RPR260243 completely reversed the action potential-prolonging effects of dofetilide in this preparation. Using the Langendorff heart method, we found that 5 μM RPR260243 increased T-wave amplitude, prolonged the PR interval, and shortened the QT interval. We believe RPR260243 represents...

Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jul.-17-2017Print Date:Jul.-17-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :TMP195Catalog No. :HY-18361CAS No. :1314891-22-91.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:N–[2–Methyl–2–(2–phenyloxazol–4–yl)propyl]–3–[5–(trifluoromethyl)–1,2,4–oxadiazol–3–yl]benzamide Formula:C23H19F3N4O3Molecular Weight:456.42CAS No. :1314891-22-94. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

=====================================================================Acq. Operator : Li Shan(LCMS-02) Seq. Line : 64Acq. Instrument : HY-LCMS-02 Location : P1-D-02Injection Date : 5/7/2015 2:55:41 PM Inj : 1Inj Volume : 3.000 µlAcq. Method : D:\AGLIENT 1260\DATA\20150507\20150507 2015-05-07 09-02-19\100-1000MS+3MIN- 1.5_(0.02%FA).MLast changed : 5/7/2015 9:02:19 AM by Li Shan(LCMS-02)Analysis Method : D:\AGLIENT 1260\METHOD\10-80A(RP-HPLC).M Last changed : 5/7/2015 3:58:57 PM by Li Shan(LCMS-02) (modified after loading)Method Info : 10-80A,16MINCatalog No : HY-13804 Batch#09735 A-RP-132Additional Info : Peak(s) manually integratedmin0.511.522.53mAU 02004006008001000 DAD1 B, Sig=214,4 Ref=off (D:\AGLIENT...0\DATA\20150507\20150507 2015-05-07 09-02-19\CPK2015-507-09735.D)1.5432.1752.381===================================================================== Area Percent Report =====================================================================Sorted By : Signal Multiplier : 1.0000Dilution : 1.0000Do not use Multiplier & Dilution Factor with ISTDsSignal 1: DAD1 B, Sig=214,4 Ref=offPeak RetTime Type Width Area Height Area # [min] [min] [mAU*s] [mAU] %----|-------|----|-------|----------|----------|--------| 1 1.543 MM 0.0881 6.48576 1.22727 0.1260 2 2.175 MM 0.0795 5132.37061 1075.95581 99.6765 3 2.381 MM 0.0656 10.17070 2.58434 0.1975Totals : 5149.02707 1079.76743===================================================================== *** End of Report ***============================================================Acq. Operator : Li Shan(LCMS-02) Seq. Line : 64Acq. Instrument : HY-LCMS-02 Location : P1-D-02Injection Date : 5/7/2015 2:55:41 PM Inj : 1Inj Volume : 3.000 µlAcq. Method : D:\AGLIENT 1260\DATA\20150507\20150507 2015-05-07 09-02-19\100-1000MS+3MIN- 1.5_(0.02%FA).MLast changed : 5/7/2015 9:02:19 AM by Li Shan(LCMS-02)Analysis Method : D:\AGLIENT 1260\METHOD\10-80A(RP-HPLC).M Last changed : 5/7/2015 4:00:08 PM by Li Shan(LCMS-02) (modified after loading)Method Info : 10-80A,16MINCatalog No : HY-13804 Batch#09735 A-RP-132Additional Info : Peak(s) manually integratedmin0.511.522.53100000200000300000400000500000600000700000 MSD1 TIC, MS File (D:\AGLIENT 1260\DATA\20150507\20150507 2015-05-07 09-02-19\CPK2015-507-09735.D) ES-API, Pos, Sc2.166MS Signal: MSD1 TIC, MS File, ES-API, Pos, Scan, Frag: 50 Spectra averaged over upper half of peaks. Noise Cutoff: 1000 counts.Reportable Ion Abundance: > 10%.Retention Mol. Weight Time (MS) MS Area or Ion2.166 6081498 282.90 I 281.95 Im/z100200300400500600700020406080100*MSD1 SPC, time=2.127:2.218 of D:\AGLIENT 1260\DATA\20150507\20150507 2015-05-07 09-02-19\CPK2015-507-09735.D ES-API Max: 506720282.9 282.0*** End of Report ***。