SCH79797 dihydrochloride [1216720-69-2]

Cat# T12870-10mg

Size : 10mg

Marca : TargetMol


SCH79797 dihydrochloride

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SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.
SCH79797 dihydrochloride
Cas No. 1216720-69-2
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.5%
Appearance:Solid
Color:White
COA LCMS HNMR

Product Introduction

Bioactivity
Description
SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.
In vitro
SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. In NIH 3T3 cells, SCH79797 dihydrochloride inhibits serum-stimulated activation of p44/p42 mitogen-activated protein kinases (MAPK) at low concentrations and induces apoptosis at higher concentrations[1]. SCH79797 dihydrochloride inhibits high-affinity thrombin receptor-activating peptide ([3H]haTRAP) binding in a competitive manner. SCH79797 dihydrochloride inhibits α-thrombin- and haTRAP-induced aggregation of human platelets. Thrombin produces transient increases in cytosolic free Ca2+ concentration ([Ca2+]i) in hCASMC. SCH79797 dihydrochloride effectively inhibits this increase in [Ca2+]i. SCH79797 dihydrochloride completely inhibits Thrombin- and TK-stimulated [3H]thymidine incorporation [4].
In vivo
In male Sprague Dawley rats, SCH79797 dihydrochloride (2.5 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 100 μg/kg, and 250 μg/kg; i.v.) reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury immediately before or during ischemia[3].
Chemical Properties
Molecular Weight444.4
FormulaC23H27Cl2N5
Cas No.1216720-69-2
SmilesCl.Cl.CC(C)c1ccc(Cn2ccc3c2ccc2nc(NC4CC4)nc(N)c32)cc1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 10 mg/mL (22.5 mM), Sonication and heating are recommended.
DMSO: 50 mg/mL (112.51 mM), Sonication and heating are recommended.
In Vivo Formulation
10% DMSO+90% Saline: 5 mg/mL (11.25 mM), Suspension.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.2502 mL11.2511 mL22.5023 mL112.5113 mL
5 mM0.4500 mL2.2502 mL4.5005 mL22.5023 mL
10 mM0.2250 mL1.1251 mL2.2502 mL11.2511 mL
20 mM0.1125 mL0.5626 mL1.1251 mL5.6256 mL
DMSO
1mg5mg10mg50mg
50 mM0.0450 mL0.2250 mL0.4500 mL2.2502 mL
100 mM0.0225 mL0.1125 mL0.2250 mL1.1251 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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