產(chǎn)品目錄

規(guī)格	10mg 50mg 100mg
CAS	1289023-67-1
別名	BMS 927711;BMS927711
化學(xué)名	5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate
分子式	C28H28F2N6O3
分子量	534.56
溶解度	DMF: 5 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

BMS-927711 is an orally potent CGRP receptor antagonist with IC50 of 0.14 nM. [1]

Calcitonin gene-related peptide CGRP is a 37 amino acid peptide widely distributed in the nervous system, which is a highly potent vasodilator that has been directly implicated in the pathology of migraine. Studies have revealed that plasma concentrations of CGRP are elevated during migraine attacks, and these levels could be normalized by sumatriptan in connection with the relief of headache. CGRP receptors are G-coupled cell surface receptors composed of the calcitonin receptor-like receptor (CLR), receptor activity modifying protein 1 (RAMP1), and the receptor component protein (RCP). BMS-927711 is an antagonist of CGRP receptor and could alleviate migraine. [1, 2]

Binding affinities for the human CGRP receptor were determined by inhibition of 125I-CGRP binding to SK-N-MC cell membranes, which endogenously express receptor. BMS-927711 was shown to be a full, competitive antagonist with IC 50 = 0.14±0.01 nM. Moreover, it showed excellent permeability in tests of PAMPA. Functional receptor antagonism for BMS-927711 was determined by measuring inhibition of CGRP-stimulated cAMP production in SK-N-MC cells. [1]

In a large Phase 2b study testing BMS-927711 for the acute treatment of migraine, an adaptive design to test six doses of BMS-927711 (10, 25, 75, 150, 300 and 600 mg) against placebo was adopted while Sumatriptan 100 mg was used as an active comparator. BMS-927711 was proved to be effective at multiple doses. For the primary endpoint, namely the proportion pain-free at 2 hours post dose, doses of 75 mg, 150 mg and 300 mg (as well as sumatriptan) were superior to placebo. However, 600mg showed no additional benefits over lower doses. Besides, efficacy was numerically inferior to sumatriptan for this endpoint for all doses. [2]

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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