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Olcegepant

Catalog No. T12293L CAS 204697-65-4

Synonyms: BIBN-4096, BIBN 4096BS

Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).

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Olcegepant, CAS 204697-65-4

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1 mg	In stock	$ 31.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 97.00
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50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 199.00

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Purity: 96.08%

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Description	Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).
Targets&IC50	CGRP1:0.03 nM, CGRP (human):14.4 pM (ki)
In vitro	Olcegepant exhibits exceptional efficacy at primate CGRP receptors, demonstrating a high affinity (Ki) of 14.4±6.3 (n=4) pM for human CGRP receptors, surpassing that of the endogenous ligand CGRP and demonstrating a 150-fold greater affinity than the peptidic antagonist CGRP8-37. It competitively antagonizes CGRP-induced concentration-dependent relaxation, effectively reversing CGRP-mediated vasodilation in human cerebral vessels and inhibiting neurogenic vasodilation in a surrogate animal model for migraine pathophysiology. This suggests that Olcegepant, acting as a CGRP receptor antagonist, may be a potential novel abortive treatment for migraines. Its competitive antagonism has also been confirmed in SK-N-MC cells, with its effects observed in isolated human cerebral, coronary, and omental arteries using sensitive myograph techniques[1][2][3].
In vivo	Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. The expression of the phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment. Olcegepant in doses between 1 and 30 μg/kg (i.v.) suppresses the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly decreases mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly decreases the number of c-Fos immunolabeled cells in the spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in the trigeminal ganglion of CCI-ION rats [2][4][5].

Synonyms	BIBN-4096, BIBN 4096BS
Molecular Weight	869.65
Formula	C38H47Br2N9O5
CAS No.	204697-65-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (11.50 mM), Sonification is recommended

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max Ion Channel Inhibitor Library ReFRAME Related Library Clinical Compound Library Neuronal Signaling Compound Library

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Keywords

Olcegepant 204697-65-4 GPCR/G Protein Neuroscience CGRP Receptor inhibit BIBN 4096 BIBN4096 Calcitonin gene-related peptide receptor BIBN-4096 Inhibitor BIBN 4096BS inhibitor

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