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Olcegepant

Olcegepant

产品编号 T12293L   CAS 204697-65-4
别名: BIBN-4096, BIBN 4096BS

Olcegepant (BIBN-4096) 是一种选择性的降钙素基因相关肽1 (CGRP1) 受体拮抗剂,IC50=0.03 nM,Ki=14.4 pM。

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Olcegepant Chemical Structure
Olcegepant, CAS 204697-65-4
规格 价格/CNY 货期 数量
1 mg ¥ 622 现货
2 mg ¥ 913 现货
5 mg ¥ 1,490 现货
10 mg ¥ 2,330 现货
25 mg ¥ 3,950 现货
50 mg 特惠询价 现货
1 mL * 10 mM (in DMSO) ¥ 2,230 现货
其他形式的 Olcegepant:
产品目录号及名称: Olcegepant (T12293L)
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特惠询价: Olcegepant (T12293L)
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选择批次  
纯度: 96.08%
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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 (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).
靶点活性 CGRP1:0.03 nM, hCGRP:14.4 pM (ki)
体外活性 Olcegepant is extremely effective at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM. Olcegepant possesses a higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Olcegepant shows 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[1][2][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%. The expression of the phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment. Olcegepant in doses between 1 and 30 μg/kg (i.v.) suppresses the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly decreases mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly decreases the number of c-Fos immunolabeled cells in the spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in the trigeminal ganglion of CCI-ION rats [2][4][5].
别名 BIBN-4096, BIBN 4096BS
分子量 869.65
分子式 C38H47Br2N9O5
CAS No. 204697-65-4

存储

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

溶解度

DMSO: 10 mg/mL (11.50 mM), Sonification is recommended

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1499 mL 5.7494 mL 11.4989 mL 28.7472 mL
5 mM 0.23 mL 1.1499 mL 2.2998 mL 5.7494 mL
10 mM 0.115 mL 0.5749 mL 1.1499 mL 2.8747 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

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. Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. 3. 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. 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. 5. Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153(9):1939-48.
Rimegepant ML230 Adrenomedullin (AM) (22-52), human acetate Vazegepant hydrochloride CGRP antagonist 1 Ubrogepant Galcanezumab β-CGRP, human acetate

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 ReFRAME 相关化合物库 GPCR靶点分子库 神经信号分子库 已知活性化合物库 药物功能重定位化合物库 抑制剂库 离子通道库 经典已知活性库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
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。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Olcegepant 204697-65-4 GPCR/G Protein Neuroscience CGRP Receptor inhibit BIBN 4096 BIBN4096 Calcitonin gene-related peptide receptor BIBN-4096 Inhibitor BIBN 4096BS inhibitor

 

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