RS-127445
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) .
Product Specifications
CAS Number
199864-87-4
Product Name Alternative
RS-127445 | RS127445 | MT-500
Purity
>98% (HPLC)
Smiles
CC (C) C1=NC (N) =NC (=C1) C1=C2C=CC=CC2=C (F) C=C1
Molecular Formula
C17H16FN3
Molecular Weight
281.33
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Amino-4- (4-fluoronaphth-1-yl) -6-isopropylpyrimidine
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