Olcegepant
Cat.No:IO2560 Solarbio
CAS:204697-65-4
Purity:≥96%
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My CartCAS:204697-65-4
Purity:≥96%
Qty:
Size:
CAS | 204697-65-4 |
Name | Olcegepant |
Purity | ≥96% |
Target Point | CGRP Receptor |
Passage | GPCR & G Protein |
Background | Olcegepant is a potent and selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist. |
Biological Activity | Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.[1-5] |
IC50 | IC50: 0.03 nM (CGRP1)[1]Ki: 14.4 pM (hCGRP)[2] |
Data Literature Source | [1]. Rudolf K, et al. Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem.?2005 Sep 22;48(19):5921-31. [2]. Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. [3]. Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. [4]. Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132(Pt 11):3134-41. [5]. Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153(9):1939-48. |
Unit | Bottle |
Specification | 1mg |
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
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