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SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonist with an IC50=70 nM with antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects that attenuates thrombin-induced increase in CH25H expression in astrocytes, inhibits peritoneal dissemination of gastric cancer, and attenuates repetitive traumatic brain injury.


| Description | SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonist with an IC50=70 nM with antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects that attenuates thrombin-induced increase in CH25H expression in astrocytes, inhibits peritoneal dissemination of gastric cancer, and attenuates repetitive traumatic brain injury. |
| Targets&IC50 | PAR1:70 nM, PAR1:35 nM ( ki) |
| In vivo | Methods: SCH79797 (2.5, 10, 25, 50, 100 and 250 μg/kg, intravenously) was administered to rats and subjected to 30 min of ischemia and 180 min of reperfusion to investigate its cardioprotective effects in vivo. Results: Infarct size, expressed as a percentage of area at risk (AAR), was 62 ± 3 % of the AAR in the control group; no significant changes in infarct size were observed at the lowest (2.5 μg/kg) and highest (250 μg/kg) doses of SCH79797; however, a gradual decrease was observed at doses of 10-100 μg/kg, with 25 μg/kg being the most effective dose. [1] |
| Synonyms | SCH-79797, SCH 79797 |
| Molecular Weight | 371.48 |
| Formula | C23H25N5 |
| Cas No. | 245520-69-8 |
| Smiles | N=1C(=NC2=CC=C3C(C=CN3CC4=CC=C(C=C4)C(C)C)=C2C1N)NC5CC5 |
| Relative Density. | 1.32 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (107.68 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.38 mM), Sonication is recommended. 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 | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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