Atopaxar hydrobromide

SKU: orb1225003

Description

A potent, reversible PAR-1 antagonist with IC50 of 19 nM; shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC50 of 64 nM and 31 nM, respectively, with no effect on platelet aggregation induced by either ADP or collagen; inhibits arterial thrombosis without affecting bleeding time in photochemically-induced thrombosis model guinea pigs.Thrombosis Phase 2 Clinical.

Key Properties

• CAS Number: 474550-69-1
• MW: 608.54
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₈FN₃O₅.HBr
• SMILES: COC1=C(N2CCOCC2)C=C(C(CN(CC3=C4C(F)=C(OCC)C(OCC)=C3)C4=N)=O)C=C1C(C)(C)C.[H]Br
• Target: PAR
• Solubility: DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Atopaxar (30-100 mg/kg; p.o.) hydrobromide causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model. Atopaxar hydrobromide does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg. Animal model: Guinea pigs, PIT model. Dosage: Oral administration. Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg. Result: Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls.
• In Vitro:
  Atopaxar hydrobromide (0.0001-10 μM; 1h) inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC50 of 0.019 μM. Atopaxar hydrobromide shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC50s of 0.064 and 0.031 μM, respectively, but has no effect on platelet aggregation induced by either ADP or collagen. Atopaxar hydrobromide shows potent and selective inhibitory effects on guinea pig platelet aggregation induced by thrombin and TRAP with IC50s of 0.13 and 0.097 μM, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E5555 hydrobromide

Quick Database Links

Gene Symbol

PAR