Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (11.50 mM), Sonification is recommended
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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