2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. Protease-Activated Receptor-1 antagonist 2

Protease-Activated Receptor-1 antagonist 2 

Cat. No.: HY-143314
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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.

Protease-Activated Receptor-1 antagonist 2 Chemical Structure

Protease-Activated Receptor-1 antagonist 2 Chemical Structure

CAS No. : 1454588-34-1

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Protease-Activated Receptor-1 antagonist 2 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 7 nM (PAR-1)[1].
In Vivo

Protease-Activated Receptor-1 antagonist 2 (Compound 14, 1 mpk i.v. dosing, rat and monkey) inhibits PAR-1 with an IC50 of 7 nM[1].
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.

Animal Model: Rat, monkey, dog[1]
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)
Administration: i.v., p.o (Pharmacokinetic Analysis)
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
Molecular Weight

423.46

Formula

C24H23F2N3O2
CAS No.
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
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
References
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Protease-Activated Receptor-1 antagonist 2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Protease-Activated Receptor-1 antagonist 21454588-34-1Protease Activated Receptor (PAR)Thrombin receptorsProtease-Activated Receptor-1PAR-1 AntagonistatherosclerosisrestenosisInhibitorinhibitorinhibit

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