ChemicalBook CAS DataBase List 1478711-48-6

1478711-48-6

Name	Benzamide, 4-[4-[[[6-methoxy-2-(2-methoxyimidazo[2,1-b]-1,3,4-thiadiazol-6-yl)-4-benzofuranyl]oxy]methyl]-2-thiazolyl]-N,N-dimethyl-
CAS	1478711-48-6
Molecular Formula	C27H23N5O5S2
Molecular Weight	561.63
MOL File	1478711-48-6.mol

Chemical Properties

density	1.47±0.1 g/cm3(Predicted)
form	Solid
pka	0.52±0.50(Predicted)
color	White to off-white

Hazard Information

Uses

BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect[1][2].

in vivo

BMS-986141 (compound 49) shows a slight but significant prolongation of KBT (kidney bleeding time) and demonstrates excellent anti-thrombotic efficacy at 0.5 mg/kg in cynomolgus monkey^[1]^[2].

Animal Model:	Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models^[2]
Dosage:	0.05, 0.1, 0.5 mg/kg
Administration:	p.o., 2 hours
Result:	Inhibited PAR4-AP-induced platelet aggregation in human and monkey blood with IC50 of 1.8 and 1.3 nM, respectively. Reduced the thrombus weight by 36%, 63% and 88% at concentrations of 0.05, 0.1 and 0.5 mg/kg, respectively in AT model. Increased MBT by 1.2 times.

Animal Model:

Rat, dog and monkey^[1]

Dosage:

0.5, 1, 2 mpk

Administration:

i.v., 0.5 mpk, 10 min or p.o., 2 mpk for rat, 1 mpk for dog and monkey

Result:

The pharmacokinetic parameters of BMS-986141 (compound 49)

Parameters	rat	dog	monkey
t_1/2(h)	3.7 ± 0.4	13	75 ± 12
CL (mL/min/kg)	14.3 ± 0.4	8.5	12 ± 2
Vss(L/kg)	2.7 ± 0.3	2.7	14 ± 5
F (%)	31	25	36

IC 50

PAR4: .4 nM (IC₅₀)

References

[1] E Scott Priestley, et al. Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4. J Med Chem. 2022 Jul 14;65(13):8843-8854. DOI:10.1021/acs.jmedchem.2c00359
[2] P Wong, et al. Favorable therapeutic index of an orally-active small-molecule antagonist of the platelet protease-activated receptor-4, BMS-986141, compared with the P2Y12 antagonist ticagrelor in cynomolgus monkeys. European Heart Journal, Volume 41, Issue Supplement_2, November 2020.

Spectrum Detail

Supplier

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