RS-127445

Overview
Catalog #	bs-6600c-10mg-solid
Product Name	RS-127445
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 281.33 Formula: C17 H16 F N3 CAS Number: 199864-87-4 InChi Key: ZZZQXCUPAJFVBN-UHFFFAOYSA-N InChi: InChI=1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21) Smiles: CC(C)C1=CC(=NC(N)=N1)C1=CC=C(F)C2=CC=CC=C21 Purity: 98.0 Solubility: DMSO: 56 mg/mL(199.05 mM). Water: Insoluble. Appearance: Solid Power. Shelf Life: 1.0 years
Description	RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1, 000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3).