CAS NO: | 204697-65-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of thecalcitoningene-related peptide 1 (CGRP1) receptorwithIC50of 0.03 nM andKiof 14.4 pM for human CGRP[1][2]. | ||||||||||||||||
IC50& Target | IC50: 0.03 nM (CGRP1)[1] | ||||||||||||||||
体外研究 (In Vitro) | Olcegepant possesses higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology[1]. 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]. | ||||||||||||||||
体内研究 (In Vivo) | Olcegepant (BIBN4096BS) in doses between 1 and 30 μg/kg (i.v.) inhibits the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys[2]. 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]. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly reduces mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly reduces the number of c-Fos immunolabeled cells in spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in trigeminal ganglion of CCI-ION rats[5]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 869.65 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C38H47Br2N9O5 | ||||||||||||||||
CAS 号 | 204697-65-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
| ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(57.49 mM) 1M HCl : 50 mg/mL(57.49 mM;ultrasonic and adjust pH to 1 with HCl) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|