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586368-06-1

中文名稱 586368-06-1
英文名稱 Olcegepant (hydrochloride)
CAS 586368-06-1
更新日期 2023/03/20 15:41:25
分子式 C38H48Br2ClN9O5
分子量 906.12
MOL 文件 586368-06-1.mol
586368-06-1 結(jié)構(gòu)式 586368-06-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12293
英文別名
BIBN-4096 hydrochloride
BIBN4096BS hydrochloride
BIBN-4096BS hydrochloride
BIBN 4096BS hydrochloride
Olcegepant (hydrochloride)
BIBN-4096 HYDROCHLORIDE
BIBN-4096BS HYDROCHLORIDE
BIBN4096BS HYDROCHLORIDE
BIBN 4096BS HYDROCHLORIDE

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
形態(tài)Solid
顏色Light yellow to yellow
水溶解性Water: ≥ 66.66 mg/mL (73.57 mM)
586368-06-1價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/05HY-10095A586368-06-1
Olcegepant hydrochloride
586368-06-12mg1100元
2025/02/05HY-10095A586368-06-1
Olcegepant hydrochloride
586368-06-15mg1888元
2025/02/05HY-10095A586368-06-1
Olcegepant hydrochloride
586368-06-110mM * 1mLin DMSO2910元

常見問題列表

生物活性
Olcegepant hydrochloride (BIBN-4096 hydrochloride) 是高效選擇性的降鈣素基因相關(guān)肽 (CGRP) 的拮抗劑, 對人類CGRP的 Ki 值為 14.4 pM。
靶點

IC50: 0.03 nM (CGRP1)
Ki: 14.4 pM (hCGRP)

體外研究

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.

體內(nèi)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.

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