Olcegepant

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Chemical Structure| 204697-65-4 同义名 : BIBN-4096; BIBN 4096BS
CAS号 : 204697-65-4
货号 : A757427
分子式 : C38H47Br2N9O5
纯度 : 98+%
分子量 : 869.64
MDL号 : MFCD07772306
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(57.49 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

1M HCl: 50 mg/mL(57.49 mM)，配合低频超声，并调节pH至1
生物活性
描述 Olcegepant is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor (IC50= 0.03 nM).
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.11mL

5.75mL

1.15mL

0.57mL

11.50mL

2.30mL

1.15mL
参考文献

[1]Rudolf K, Eberlein W, et al. Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl] carbonyl] -D-tyrosyl] -l-lysyl] -4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem. 2005 Sep 22;48(19):5921-31.

[2]Doods H, Hallermayer G, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3.