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

Protease-Activated Receptor-1 antagonist 2 

Cat. No.: HY-143314
Handling Instructions

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

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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) ex vivo platelet agg % eff @ 1/0.3 mpk (t, h) hERG IC50 (μM) Pgp (BA/AB) H; R; control Pappb Hep Cl (μL/min/106 cells) R; D; M; H Cl (mL/min/kg) (R;c D; d Me) CLU (mL/min/kg) (R;c D; d Me) Vd (L/kg) (R;c D; d Me) Vd,U (L/kg) (R;c D; d Me) fU, plasma (L/kg) (R; D; M) MRT (R;c D; d Me) F% (R;f D; g Mh) predicted human MRT Panlabs (Disc. Sci)
Protease-Activated Receptor-1 antagonist 2 7 100 (24)/100 (24) >60 1.1; 2.6; 0.6 Molecular Weight

423.46

Formula

C24H23F2N3O2

CAS No.
SMILES

[H][[email protected]]12[[email protected]]([[email protected]@H](C(F)(C[[email protected]]1(C(O[[email protected]@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.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Protease-Activated Receptor-1 antagonist 2
Cat. No.:
HY-143314
Quantity:
MCE Japan Authorized Agent: