2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. PAR4 antagonist 7

PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice.

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PAR4 antagonist 7 Chemical Structure

PAR4 antagonist 7 Chemical Structure

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PAR4 antagonist 7 Related Antibodies

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Description

PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice[1].

In Vitro

PAR4 antagonist 7 inhibits PAR4 agonist peptide (PAR4-AP) (75 μM)-induced washed platelet (WP) aggregation, with an IC50 of 15.32 nM[1].
PAR4 antagonist 7 inhibits PAR4-AP (75 μM) induced human platelet-rich plasma (PRP) levels, with an IC50 of 6.39 nM[1].
PAR4 antagonist 7 also inhibits AYPGKF-NH2 (75 μM) or Thrombin (0.1 U/mL) induced platelet aggregation of human PRP, and does not affect SFLLRN-NH2 (5 μM), Collagen (10 mg/mL), ADP (10 μM), or the U46619 (HY-108566) (3 μM) induced platelet aggregation[1].
PAR4 antagonist 7 shows excellent metabolic stability in human liver microsomes (T1/2 = 249.83 min[1].

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

PAR4 antagonist 7 Related Antibodies
In Vivo

PAR4 antagonist 7 (2.5-10 mg/kg, oral gavage) does not show a bleeding tendency in mice, could potentially address concerns regarding bleeding risks[1].
PK properties of PAR4 antagonist 7 in rats (compound 20f)

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

Dose (mg/kg) AUC(0-last) (h × ng/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) CL (mL/min/kg) F (%)
i.v. (0.5 mg/kg) 636 5.13 0.08 394 12.8
p.o. (2 mg/kg) 1217 5.16 1.67 214 25.4 50.5
Molecular Weight

541.55

Formula

C28H20FN5O4S
SMILES

COC1=NC2=CC(C)=CC(C3=NC4=C(S3)C(C[C@@H](O5)COC(NC6=CC=CC(C#N)=C6)=O)=C5C(F)=C4)=C2C=N1
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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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PAR4 antagonist 7 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:

PAR4 antagonist 7Protease Activated Receptor (PAR)Thrombin receptorsplatelet aggregationCoronary artery diseaseantiplateletBleeding riskInhibitorinhibitorinhibit

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PAR4 antagonist 7
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