Atopaxar

CAS NO.：751475-53-3
Empirical Formula: C29H38FN3O5
Molecular Weight: 527.63
MDL number: MFCD20040417
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-19 15:53:33

What is Atopaxar?

Definition

ChEBI: Atopaxar is an aromatic ketone.

Biological Activity

Atopaxar (E5555) is a potent, orally active, selective, reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. It can be used in the study of atherothrombotic diseases and interferes with platelet signaling..

in vitro

Atopaxar inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC ₅₀ of 0.019 μM. < br/> Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner.
Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM.

in vivo

Atopaxar (30-100 mg/kg; po) causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model.
Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg.

< td class="col1 fwb"> Result:

Animal Model:	Guinea pigs, PIT model
Dosage:	Oral administration
Administration:	10 mg/kg, 30 mg/kg, 100 mg/kg
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.

Properties of Atopaxar

Boiling point:	671.0±65.0 °C(Predicted)
Density	1.22
storage temp.	Store at -20°C
solubility	DMSO : 250 mg/mL (473.82 mM; Need ultrasonic)
pka	7.43±0.20(Predicted)
form	Solid
color	White to off-white