586368-06-1
- CAS号:586368-06-1
- 英文名:Olcegepant (hydrochloride)
- 中文名:586368-06-1
- CBNumber:CB03167627
- 分子式:C38H48Br2ClN9O5
- 分子量:906.12
- MOL File:586368-06-1.mol
- 储存条件 :Store at -20°C
- 形态 :Solid
- 颜色 :Light yellow to yellow
- 水溶解性 :Water: ≥ 66.66 mg/mL (73.57 mM)
586368-06-1性质、用途与生产工艺
- 生物活性 Olcegepant hydrochloride (BIBN-4096 hydrochloride) 是高效选择性的降钙素基因相关肽 (CGRP) 的拮抗剂, 对人类CGRP的 Ki 值为 14.4 pM。
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靶点
IC50: 0.03 nM (CGRP1)
Ki: 14.4 pM (hCGRP) -
体外研究
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.
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体内研究
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.
- 更新日期:2024/04/30
- 产品编号:HY-10095A
- 产品名称:586368-06-1 Olcegepant hydrochloride
- CAS编号:586368-06-1
- 包装:2mg
- 价格:1100元
- 更新日期:2024/04/30
- 产品编号:HY-10095A
- 产品名称:586368-06-1 Olcegepant hydrochloride
- CAS编号:586368-06-1
- 包装:5mg
- 价格:1888元
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