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586368-06-1

586368-06-1, 586368-06-1, 結(jié)構(gòu)式
586368-06-1
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

586368-06-1化學(xué)性質(zhì)

儲存條件:
Store at -20°C
形態(tài):
Solid
顏色:
Light yellow to yellow
水溶解性:
Water: ≥ 66.66 mg/mL (73.57 mM)
安全信息

586368-06-1性質(zhì)、用途與生產(chǎn)工藝

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.

586368-06-1 上下游產(chǎn)品信息

上游原料

下游產(chǎn)品

586368-06-1 試劑級價格

更新日期產(chǎn)品編號產(chǎn)品名稱CAS編號包裝價格
2024/11/08HY-10095A586368-06-1
Olcegepant hydrochloride
586368-06-12mg1100元
2024/11/08HY-10095A586368-06-1
Olcegepant hydrochloride
586368-06-15mg1888元

586368-06-1 生產(chǎn)廠家

全球有 15家供應(yīng)商   586368-06-1國內(nèi)生產(chǎn)廠家
供應(yīng)商聯(lián)系電話電子郵件國家產(chǎn)品數(shù)優(yōu)勢度
上海昂提生物科技有限公司 13764913901 info@angtibio.com 中國 5028 55
上海晶石醫(yī)藥科技有限公司 021-000000 admin@jingshipharmatech.com 中國 9986 58
范德(北京)生物科技有限責(zé)任公司 15911056312 liming@bio-fount.com 中國 9729 58
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美國 32161 58
BOC Sciences info@bocsci.com 美國 0 65
上海源溪生物科技有限公司 021-58447131 13564518121 sales@dcchemicals.com 中國 9409 58
愛必信(上海)生物科技有限公司 021-38015121 15000105423 wulan@absin.cn 中國 24731 58
天津普西唐生物醫(yī)藥科技有限公司 010-60605840 15801484223 psaitong@jm-bio.com 中國 29774 58
開封明仁藥業(yè)有限公司 0371-65741762 sales@hasunny.com 中國 2380 58
上海陌孚醫(yī)藥科技有限公司 021-59167510 18117107507 vip@med-life.cn 中國 4997 58
南京世洲生物科技有限公司 025-85560043 15850508050 cindy.huang@synzest.com 中國 12000 58
Aladdin Scientific +1-+1(833)-552-7181 sales@aladdinsci.com 美國 52924 58
 

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)
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