Protease-Activated Receptor-1 antagonist 2
Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis.
For research use only. We do not sell to patients.
- CAS No.: 1454588-34-1
- Formula: C24H23F2N3O2
- Molecular Weight:423.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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PAR1 7 nM (IC50) |
Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC0?24 h and Cmax in a dose-dependent manner[1].
Protease-Activated Receptor-1 antagonist 2 doesn’t elicit any prominent liver bioactivation or tissue toxicity signals up to an AUC of 44 μM?h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat, monkey, dog[1]
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Dosage:i.v. (3 mpk for rat, 0.3 mpk for dog and monkey), p.o (10 mpk for rat, 1 mpk for dogs and monkey)
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Administration:i.v., p.o (Pharmacokinetic Analysis)
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Result:Pharmacokinetic parameters.
compound FLIPR IC50 (nM) MRT (R;c D; d Me) F% (R;f D; g Mh) predicted human MRT Protease-Activated Receptor-1 antagonist 2 7 1.9; 18; 25 54; 100; 37 20−48
Chemical Information
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CAS No. 1454588-34-1
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Molecular Weight 423.46
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Formula C24H23F2N3O2
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SMILES
[H][C@]12[C@H]([C@@H](C(F)(C[C@]1(C(O[C@@H]2C)=O)N)F)C)/C=C/C3=CC=C(C=N3)C4=CC=CC=C4C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)