586368-06-1
![586368-06-1 结构式](https://www.chemicalbook.com/CAS/20211123/GIF/586368-06-1.gif)
基本信息
BIBN4096BS hydrochloride
BIBN-4096BS hydrochloride
BIBN 4096BS hydrochloride
Olcegepant (hydrochloride)
BIBN-4096 HYDROCHLORIDE
BIBN-4096BS HYDROCHLORIDE
BIBN4096BS HYDROCHLORIDE
BIBN 4096BS HYDROCHLORIDE
物理化学性质
储存条件 | -20°C储存 |
形态 | Solid |
颜色 | Light yellow to yellow |
水溶解性 | Water: ≥ 66.66 mg/mL (73.57 mM) |
586368-06-1价格(试剂级)
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/04/30 | HY-10095A | 586368-06-1 Olcegepant hydrochloride | 586368-06-1 | 2mg | 1100元 |
2024/04/30 | HY-10095A | 586368-06-1 Olcegepant hydrochloride | 586368-06-1 | 5mg | 1888元 |
2024/04/30 | HY-10095A | 586368-06-1 Olcegepant hydrochloride | 586368-06-1 | 10mM * 1mLin DMSO | 2910元 |
常见问题列表
IC50: 0.03 nM (CGRP1)
Ki: 14.4 pM (hCGRP)
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. Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (K i ) for human CGRP receptors of 14.4±6.3 (n=4) pM. 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.
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. 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. 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.