Protease-Activated Receptor-1 antagonist 3

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Data Sheet Handling Instructions

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Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC₅₀ value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K⁺ channel with an IC₅₀ value of 9 µM.

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Protease-Activated Receptor-1 antagonist 3 Chemical Structure

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•Related Small Molecules:

•Related Proteins:

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View All Isoforms

PAR1 PAR2 PAR4

Biological Activity
Purity & Documentation
References
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Description

In Vivo

Protease-Activated Receptor-1 antagonist 3 (compound 23) (3 mg/kg; i.v.) shows 10% bioavailability in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Rats^[1]
Dosage:	3 mg/kg
Administration:	I.v.
Result:	Exhibited relatively high unbound clearance values with CL_u of 742 mL/min/kg, and V_d of 1.2 L/kg in rats.

Molecular Weight

498.62

Formula

C₃₀H₃₄N₄O₃

SMILES

[H][C@]12[C@H]([C@@H]([C@@H](C)[C@H]3[C@]1(C(O[C@@H]2C)=O)CN(C(NCC)=O)C3)C)/C=C/C4=CC=C(C=N4)C5=CC=CC=C5C#N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mandal M, et al. Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery. J Med Chem. 2022 Apr 14;65(7):5575-5592. [Content Brief]