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Olcegepant  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥50mg/mL）
产品描述：基本信息 产品编号： O10260 产品名称： Olcegepant CAS: 204697-65-4   储存条件 粉末 -20℃ 四年     分子式： C38H47Br2N9O5 溶于液体 -80℃ 6个月 分子量： 869.65 -20℃ 1个月 化学名：  N-[(2R)-1-[[(2S)-6-amino-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)hexan-2-yl]amino]-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxopropan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.1499mL 5.7494mL 11.4989mL 5mM 0.2300mL 1.1499mL 2.2998mL 10mM 0.1150mL 0.5749mL 1.1499mL   生物活性 产品描述 一种有效和选择性的降钙素基因相关肽1 (CGRP1) 受体拮抗剂，IC50 和 Ki 分别为0.03nM，14.4pM。 靶点 IC50:0.03nM (CGRP1) Ki:14.4pM (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 (Ki) 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 30μg/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 (900μg/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 0.9mg/kg,i.v.) markedly reduces mechanical allodynia in CCI-ION rats.Olcegepant (0.6mg/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.   推荐实验方法(仅供参考) 激酶实验： 125I-hCGRP is used as the radioligand.The incubation buffer contained (in mM):Tris 50,NaCl 150,MgCl25 and EDTA 1,(ethylene diamine tetra-acetic acid) pH 7.4.Membrane homogenates are incubated for 180 min at room temperature with 50pM 125I-hCGRP and increasing concentrations of Olcegepant (BIBN4096BS).The incubation is terminated by filtration through GF/B glass fibre filters using a cell harvester.The protein-bound radioactivity is determined in a gamma counter.The nonspecific binding is defined as radioactivity bound in the presence of 1μM CGRP.The IC50 values are obtained by non-linear regression analysis on the basis of a one binding site model .   细胞实验:   Cells are washed with phosphate-buffered saline then pre-incubated with 300μM isobutylmethylxanthine in serum-free MEM for 30 min at 37℃ α-CGRP-(S-37) or Olcegepant (BIBN4096BS) is added and the cells are incubated for 10 min before the addition of CGRP.The incubation is continued for another 15 min,then the cells are washed with PBS and processed for cAMP determination.Maximal stimulation over basal is defined by using 100nM CGRP.Dose–response curves are generated by using Prism.   动物实验:   Rats are treated acutely with Olcegepant (0.3,0.6,and 0.9mg/kg,intravenously [i.v.] in a tail vein),GR-85548A (0.1 and 0.3mg/kg subcutaneously [s.c.]),or their respective vehicle.For combined treatment,Olcegepant (0.3mg/kg,i.v.) is administered 30 minutes before GR-85548A (0.1mg/kg,s.c.).The doses and routes of administration are based on previous reports.For subchronic treatment,CCI-ION and sham-operated rats are injected twice per day for 4 days (at 10am and 6pm) with Olcegepant (0.6mg/kg,i.v.) or its vehicle,starting on the 15th day after ligature.A further injection of Olcegepant (0.6mg/kg,i.v.) or vehicle is performed at 10am the subsequent day (19th day after ligature),just before von Frey filament testing.
保存条件：-20℃

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