204697-65-4_化工百科

中文名	Olcegepant
英文名	Olcegepant
别名	化合物OLCEGEPANT N-[2-[5-氨基-1(S)-[4-(4-吡啶基)哌嗪-1-甲酰基]戊基氨基]-1(R)-(3,5-二溴-4-羟基苄基)-2-氧代乙基]-4-(2-氧代-1,2,3,4-四氢喹唑啉-3-基)哌啶-1-甲酰胺
英文别名	BIBN-4096 Olcegepant BIBN 4096BS BIBN 4096BS API Olcegepant 1-[3,5-Dibromo-N-[[4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-1-piperidinyl]carbonyl]-D-tyrosyl-L-lysyl]-4-(4-pyridinyl)-piperazine Piperazine, 1-[3,5-dibromo-N-[[4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-1-piperidinyl]carbonyl]-D-tyrosyl-L-lysyl]-4-(4-pyridinyl)- N-[2-[5-Amino-1(S)-[4-(4-pyridinyl)piperazin-1-ylcarbonyl]pentylamino]-1(R)-(3,5-dibromo-4-hydroxybenzyl)-2-oxoethyl]-4-(2-oxo-1,2,3,4-tetrahydroquinazolin-3-yl)piperidine-1-carboxamide
CAS	204697-65-4
化学式	C38H47Br2N9O5
分子量	869.65
密度	1.497
沸点	1091.9±65.0 °C(Predicted)
酸度系数	6.80±0.25(Predicted)
存储条件	-20℃
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.
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.

204697-65-4 - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	1.15 ml	5.749 ml	11.499 ml
5 mM	0.23 ml	1.15 ml	2.3 ml
10 mM	0.115 ml	0.575 ml	1.15 ml
5 mM	0.023 ml	0.115 ml	0.23 ml

最后更新：2024-01-02 23:10:35

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CAS: 204697-65-4
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产品描述: 中文名：Olcegepant 英文名:Olcegepant CAS:204697-65-4 规格:99% 产地:中国上海

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CAS: 204697-65-4
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产品名: Olcegepant 去供应商网站查看询盘
CAS: 204697-65-4
产地: 上海
规格: 99%
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