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Olcegepant hydrochloride

产品编号 T12293 CAS 586368-06-1

别名: BIBN-4096 hydrochloride, BIBN4096BS hydrochloride

Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).

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Olcegepant hydrochloride Chemical Structure

Olcegepant hydrochloride, CAS 586368-06-1

规格	价格/CNY		货期	数量
50 mg	￥ 7,280		待询

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Olcegepant hydrochloride 的其他形式现货产品:

Olcegepant

其他形式的 Olcegepant hydrochloride:

Olcegepant
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).
靶点活性	CGRP1:0.03 nM , CGRP (human):(ki)14.4 pM
体外活性	Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM[2].?Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment.?Olcegepant (BIBN4096BS) exhibits competitive antagonism at the CGRP receptor present in SK-N-MC cells.?Isolated human cerebral, coronary, and omental arteries are studied with a sensitive myograph technique.?CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner[3].
体内活性	Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%.?In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment[4].

别名	BIBN-4096 hydrochloride, BIBN4096BS hydrochloride
分子量	906.11
分子式	C38H48Br2ClN9O5
CAS No.	586368-06-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 66.66 mg/mL (73.57 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O	1 mM	1.1036 mL	5.5181 mL	11.0362 mL	27.5905 mL
	5 mM	0.2207 mL	1.1036 mL	2.2072 mL	5.5181 mL
	10 mM	0.1104 mL	0.5518 mL	1.1036 mL	2.759 mL
	20 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3795 mL
	50 mM	0.0221 mL	0.1104 mL	0.2207 mL	0.5518 mL

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参考文献

1. Rudolf K, 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. Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. 3. Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. 4. Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132(Pt 11):3134-41.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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