RS-127445

Research use only, not for human use.

RS-127445 is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

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).

RS-127445; RS127445; MT-500

Others

Other Targets

5-HT2B; 5-HT2B

Neurological Disease

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199864-87-4

281.33

C17H16FN3

98%

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CC(C)C1=NC(N)=NC(=C1)C1=C2C=CC=CC2=C(F)C=C1

2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine

(-20℃)

With Ice Pack

≥ 2 years