Nastorazepide_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Oct.-08-2018Print Date:Oct.-08-20181. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :AzilsartanCatalog No. :HY-14914CAS No. :147403-03-01.2 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 mixtureGHS Classification in accordance with 29 CFR 1910 (OSHA HCS)Acute toxicity, Oral (Category 4), H302Acute aquatic toxicity (Category 1), H400Chronic aquatic toxicity (Category 1), H4102.2 GHS Label elements, including precautionary statementsPictogramSignal word WarningHazard statement(s)H302 Harmful if swallowed.H410 Very toxic to aquatic life with long lasting effects.Precautionary statement(s)P264 Wash skin thoroughly after handling.P270 Do not eat, drink or smoke when using this product.P273 Avoid release to the environment.P301 + P312 IF SWALLOWED: Call a POISON CENTER or doctor ⁄ physician if you feel unwell.P330 Rinse mouth.P391 Collect spillage.P501 Dispose of contents ⁄ container to an approved waste disposal plant.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:TAK 536;TAK536;TAK-536Formula:C25H20N4O5Molecular Weight:456.45CAS No. :147403-03-04. 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.IMDGUN number: 3077Class: 9Packing group: IIIEMS-No: F-A, S-FProper shipping name: ENVIRONMENTALLY HAZARDOUS SUBSTANCE, SOLID, N.O.S.Marine pollutant: Marine pollutantIATAUN number: 3077Class: 9Packing group: IIIProper shipping name: Environmentally hazardous substance, solid, n.o.s.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 2018 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。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:CCCP inhibits STING–mediated IFN–β production via disrupting mitochondrial membrane potential (MMP). CCCP inhibits activation of STING and its downstream signaling molecules, TBK1 and IRF3.IC50 & Target: STING [1]IFN–β[1]In Vitro: CCCP inhibits IFN–β production induced by various types of the STING pathway activators. CCCP suppresses thephosphorylation of STING, TBK1, and IRF3 via disrupting the association of STING and TBK1. CCCP inhibits activation of STING and its downstream signaling molecules, TBK1 and IRF3, but not STING translocation to the perinuclear region. CCCP impairs the interaction between STING and TBK1 and concomitantly triggers mitochondria fission. Importantly, the knockout of the crucialmitochondria fission regulator Drp1 restored the STING activity, indicating that CCCP down–modulates the STING pathway through DRP1–mediated mitochondria fragmentation. The protonophore CCCP that disrupts membrane potential suppresses theDMXAA–triggered STING signaling pathway. CCCP drastically suppresses the production of IFN–β in DMXAA–treated RAW264.7cells and MEFs [1].In Vivo: The same dosage of 3 mg/kg.bw each of CCCP and PPEF is used. In both the cases 1 log reduction is observed in the bacterial load. However, when 3 mg/kg.bw of PPEF is used in combination with 3 mg/kg.bw of CCCP, 6 log 10 reductionis observed in the bacterial count. The developed model validates the enhanced antibacterial activity of combinationtherapy [2].99m Tc–MIBI signals in the hearts of SD rats administered CCCP (4 mg/kg intraperitoneally) or vehicle is also measured.99m Tc–MIBI signals decrease in rat hearts administered CCCP, and the ATP content, as measured by 31P magnetic resonance spectroscopy, decreased simultaneously. To investigate whether CCCP decreased the 99m Tc–MIBI signals in rats, we analyzed the radioisotope activity of excised heart tissue from rats administered CCCP. At 180 min after 99m Tc–MIBI injection, the 99m Tc–MIBI signals from the hearts in the CCCP group are significantly lower than those in the vehicle group [3].PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[1]MEFs (5×105), Raw264.7 cells (1×106), and HeLa cells stable expressing STING (1.5×105) are stimulated with DMXAA (100 μg/mL) for 2 or 3 h, or transfected with c–di–GMP (5 μM), cGAMP (5 μg/mL), or poly (dA:dT) (2 μg/mL) for 6 h. CCCP (50 μM) is co–treated with DMXAA (100 μg/mL), or treated for the last 5 h in case of treatment of c–di–GMP or poly (dA:dT)[1].Animal Administration:[2][3]Mice [2]Female Balb/c mice n=6, per dosing group weighing 20–25 g are rendered neutropenic with 2 intraperitoneal injections ofcyclophosphamide 150 mg/kg.bw and 100 mg/kg.bw on 4 days and 1 day prior to bacterial infection. 0.1 mL of the 106 CFU/mLProduct Name:CCCP Cat. No.:HY-100941CAS No.:555-60-2Molecular Formula:C 9H 5ClN 4Molecular Weight:204.62Target:STING; IFNAR Pathway:Immunology/Inflammation; Immunology/Inflammation Solubility:DMSO: ≥ 150 mg/mLbacterial suspension is injected into right posterior thigh muscle. After 2 h post–infection mice are treated with PPEF (3 mg/kg.bw), CCCP (3 mg/kg.bw) and in combination PPEF+CCCP (3 mg/kg.bw+3 mg/kg.bw) dissolved in 0.1 mL sterile water by single bolus intravenous injection. Twenty–four hours after antibacterial administration, the mice are humanely sacrificed. Right thigh muscles from each mouse are aseptically collected, homogenized and serially diluted and processed for quantitative cultures.Rat[3]Rats are randomly divided into three groups. One group is euthanized 15 min after a dose of 12.5 MBq (337.8 μCi) 99m Tc–MIBI injection (n=6). The other two groups are administered 4 mg/kg CCCP (CCCP group; n=7) or vehicle (vehicle group; n=7) by intraperitoneal (i.p.) injection 90 min after the same dose of 99m Tc–MIBI injection and are euthanized after an additional 90 min (180 min after the 99m Tc–MIBI injection). Hearts are excised and weighed, and radioactivity is measured between 110 and 170 keV with an auto–well gamma counter. 99m Tc–MIBI signals are corrected for physical decay (half–life=6 h).References:[1]. Kwon D, et al. Carbonyl cyanide 3–chlorophenylhydrazone (CCCP) suppresses STING–mediated DNA sensing pathway through inducing mitochondrial fission. Biochem Biophys Res Commun. 2017 Aug 30. pii: S0006–291X(17)31704–7.[2]. Sinha D, et al. Synergistic efficacy of Bisbenzimidazole and Carbonyl Cyanide 3–Chlorophenylhydrazonecombination against MDR bacterial strains. Sci Rep. 2017 Mar 17;7:44419.[3]. Kawamoto A, et al. Measurement of technetium–99m sestamibi signals in rats administered a mitochondrial uncoupler and in a rat model of heart failure. PLoS One. 2015 Jan 16;10(1):e0117091.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。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.IC50 Value: 50 nM (EC50) [1]Target: TNF–alphaNecrostatin 2 is a potent in vitro necroptosis inhibitors (exemplified by 1, EC50–0.05 uM) that also were efficacious in an animal model of ischemic stroke. Many Necroptosis inhibitor derivatives are designed for researchers.Necroptosis is a regulated caspase–independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD–deficient variant of human Jurkat T cells treated with TNF–a. 5–(1H–Indol–3–ylmethyl)–2–thiohydantoins and 5–(1H–indol–3–ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins).References:[1]. Teng X, Keys H, Jeevanandam A, Structure–activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836–40.[2]. Jagtap PG, Degterev A, Choi S, Structure–activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 2007 Apr 19;50(8):1886–95.[3]. Teng X, Degterev A, Jagtap P, Structure–activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5039–44.Product Name:Necrostatin 2 (racemate)Cat. No.:HY-14622A CAS No.:852391-15-2Molecular Formula:C 13H 12ClN 3O 2Molecular Weight:277.71Target:TNF–alpha Pathway:Apoptosis Solubility:10 mM in DMSOCaution: 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。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Exatecan Mesylate (DX–8951) is a totally synthetic analogue of the topoisomerase I–inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself.IC50 value:Target: topoisomerase IExatecan was given as i.v. infusion over 30 min at a dose of 0.5mg/m2 every day for five consecutive days, repeated every 21 days.Seventy–four percentage of cycles could be given without dose or schedule modification. The main toxicity was haematotoxicity with grade 3/4 neutropenia in 49%, grade 3/4 thrombocytopenia in 23%, and grade 3/4 anaemia in 15% of patients, respectively [1]. The most common drug–related toxicity was neutropenia. Non–hematologic toxicities were mostly mild to moderate; the most common were nausea, vomiting and anorexia. Plasma concentrations of DX–8951 (the anhydrous form of DX–8951f) were well described using a linear 2–compartment PK model. All concentrations and dose events were simultaneously modeled and explained by the population PK model. There was no evidence of non–linearity in the elimination PK, auto–inhibition or induction of DX–8951 clearance over the five days of administration [2]. Thirty–one patients were treated with 100 courses of exatecan at 6 dose–schedule levels. The incidence of the principal dose–limiting toxicities, neutropenia and thrombocytopenia, was unacceptably high at exatecan doses exceeding 0.15mg/m(2)/day as a 21–day CIVI, which was determined to be the MTD for both MP and HP patients [3].References:[1]. Reichardt P, et al. Exatecan in pretreated adult patients with advanced soft tissue sarcoma: results of a phase II––study of the EORTC Soft Tissue and Bone Sarcoma Group. Eur J Cancer. 2007 Apr;43(6):1017–22.[2]. Ajani JA, et al. A phase II clinical and pharmacokinetic study of intravenous exatecan mesylate (DX–8951f) in patients with untreated metastatic gastric cancer. Invest New Drugs. 2005 Oct;23(5):479–84.[3]. Garrison MA, et al. A Phase I and pharmocokinetic study of exatecan mesylate administered as a protracted 21–day infusion in patients with advanced solid malignancies. Clin Cancer Res. 2003 Jul;9(7):2527–37.Product Name:Exatecan (Mesylate)Cat. No.:HY-13631A CAS No.:169869-90-3Molecular Formula:C 25H 26FN 3O 7S Molecular Weight:531.55Target:Topoisomerase Pathway:Cell Cycle/DNA Damage Solubility:DMSO: 15.3 mg/mLCaution: 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。