586368-06-1
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- CAS號:
- 586368-06-1
- 英文名:
- Olcegepant (hydrochloride)
- 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
- 中文名:
- 586368-06-1
- 中文別名:
- 化合物 T12293;N-((R)-1-(((S)-6-AMINO-1-OXO-1-(4-(PYRIDIN-4-YL)PIPERAZIN-1-YL)HEXAN-2-YL)AMINO)-3-(3,5-DIBROMO-4-HYDROXYPHENYL)-1-OXOPROPAN-2-YL)-4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDINE-1-CARBOXAMIDE HYDROCHLORIDE
- CBNumber:
- CB03167627
- 分子式:
- C38H48Br2ClN9O5
- 分子量:
- 906.12
- MOL File:
- 586368-06-1.mol
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586368-06-1化學(xué)性質(zhì)
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儲存條件:
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Store at -20°C
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形態(tài):
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Solid
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顏色:
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Light yellow to yellow
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水溶解性:
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Water: ≥ 66.66 mg/mL (73.57 mM)
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586368-06-1性質(zhì)、用途與生產(chǎn)工藝
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。
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
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) 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.
586368-06-1
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價格 |
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2024/11/08 | HY-10095A | 586368-06-1 Olcegepant hydrochloride | 586368-06-1 | 2mg | 1100元 |
2024/11/08 | HY-10095A | 586368-06-1 Olcegepant hydrochloride | 586368-06-1 | 5mg | 1888元 |
586368-06-1, 586368-06-1 相關(guān)搜索:
- N-((R)-1-(((S)-6-AMINO-1-OXO-1-(4-(PYRIDIN-4-YL)PIPERAZIN-1-YL)HEXAN-2-YL)AMINO)-3-(3,5-DIBROMO-4-HYDROXYPHENYL)-1-OXOPROPAN-2-YL)-4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDINE-1-CARBOXAMIDE HYDROCHLORIDE
- 化合物 T12293
- 586368-06-1
- BIBN-4096BS hydrochloride
- BIBN4096BS hydrochloride
- BIBN-4096 HYDROCHLORIDE; BIBN-4096BS HYDROCHLORIDE; BIBN4096BS HYDROCHLORIDE; BIBN 4096BS HYDROCHLORIDE
- BIBN-4096 hydrochloride
- BIBN 4096BS hydrochloride
- Olcegepant (hydrochloride)