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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
4°C, stored under nitrogen
- 英文名：
BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
586368-06-1
- 规格：
10 mM * 1 mL/2 mg/5 mg/10 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2910.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥1100.0 |
| 规格： | 5 mg | 产品价格： | ￥1888.0 |
| 规格： | 10 mg | 产品价格： | ￥2920.0 |
| 规格： | 50 mg | 产品价格： | ￥8750.0 |
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Olcegepant hydrochloride
CAS No. : 586368-06-1
MCE 国际站：Olcegepant hydrochloride
产品活性：Olcegepant hydrochloride (BIBN-4096 hydrochloride) 是高效选择性的降钙素基因相关肽 (CGRP) 的拮抗剂, 对人类CGRP的 Ki 值为 14.4 pM。
研究领域：GPCR/G Protein | Neuronal Signaling
作用靶点：CGRP Receptor
In Vitro: 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.
In Vivo: 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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文献和实验Guanidine Hydrochloride Purification of Proteins From SDS
Pepstatin A (2.0 mg/ml)10 ml Leupeptin (1.0 mg/ml)10 ml Aprotinin (5.0 mg/ml)(Protease Inhibitor Cocktail Sigma #P8340)Denaturation Buffer6 M guanidine hydrochloride 57.3 g G-HCl20 mM Hepes 7.9 2 ml 1M Hepes pH 7.910 mM KCl 0.074 g KCl0.5 mM DTT 100 ml 0.5 M
Guanidine Hydrochloride Purification of Proteins From SDS PAGE
(Sigma #P7626) 10 ml Pepstatin A (2.0 mg/ml) 10 ml Leupeptin (1.0 mg/ml) 10 ml Aprotinin (5.0 mg/ml) (Protease Inhibitor Cocktail Sigma #P8340) Denaturation Buffer 6 M guanidine hydrochloride 57.3 g G-HCl 20 mM Hepes 7.9 2 ml 1M Hepes pH 7.9 10 mM
Packed column subcritical and/or supercritical fluid chromatography (p-sub or pSFC) has been used as a powerful chiral separation technique, whereby a mobile phase produces low viscosity, a high diffusion coefficient, and a solvating power. P
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