WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 530334
Description: VU0652925 is a PAR4 antagonist. VU0652925 had a PAC1 IC50 of 43.0 pM (-pIC50±SEM: 10.4±0.04) and a P-sel IC50 of 39.2 pM (-pIC50±SEM: 10.41±0.04). PAR4 antagonists is potential useful for the development of tools such as radioligands and PET tracers that are not currently available to the field for this target.
MedKoo Cat#: 530334
Chemical Formula: C24H18N4O4S2
Exact Mass: 490.0769
Molecular Weight: 490.552
Elemental Analysis: C, 58.76; H, 3.70; N, 11.42; O, 13.05; S, 13.07
Synonym: VU0652925, VU-0652925, VU 0652925, BMS-3, BMS 3, BMS3
IUPAC/Chemical Name: 2-methoxy-6-(6-methoxy-4-((2-phenylthiazol-4-yl)methoxy)benzofuran-2-yl)imidazo[2,1-b][1,3,4]thiadiazole
InChi Key: RROGCGMHOWNSLD-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H18N4O4S2/c1-29-16-8-19(31-12-15-13-33-22(25-15)14-6-4-3-5-7-14)17-10-21(32-20(17)9-16)18-11-28-23(26-18)34-24(27-28)30-2/h3-11,13H,12H2,1-2H3
SMILES Code: COC1=NN2C(S1)=NC(C3=CC4=C(O3)C=C(OC)C=C4OCC5=CSC(C6=CC=CC=C6)=N5)=C2
1. MOL #106666; Contributions of PAR1 and PAR4 to thrombin induced GPIIbIIIa activation in human platelets; Matthew T. Duvernay, Kayla J. Temple, Jae G. Maeng, Anna L. Blobaum, Shaun R. Stauffer, Craig W. Lindsley, Heidi E. Hamm Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232-6600, USA MTD, KJT, JGM, ALB, SRS, HEH, CWL; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA KJT, ALB, SRS, CWL; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA SRS, CWJ Molecular Pharmacology Fast Forward. Published on October 26, 2016 as DOI: 10.1124/mol.116.106666
2. Preparation of protease activated receptor 4 (PAR4) agonist peptides and their use as PAR4 receptor activation for measuring the activity of PAR4 antagonist imidazothiadiazole and imidazopyridazine derivatives and analogs; Kornacker, Michael G.; Mapelli, Claudio; Riexinger, Douglas James
Assignee Bristol-Myers Squibb Company, USA; 2013; Patent Information; Oct 31, 2013; WO 2013163248 A1