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Olcegepant hydrochloride

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Catalog No. T12293Cas No. 586368-06-1
Alias BIBN4096BS hydrochloride, BIBN-4096 hydrochloride

Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).

Olcegepant hydrochloride

Olcegepant hydrochloride

😃Good
Catalog No. T12293Alias BIBN4096BS hydrochloride, BIBN-4096 hydrochlorideCas No. 586368-06-1
Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).
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Product Introduction

Bioactivity
Description
Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).
Targets&IC50
CGRP1:0.03 nM , CGRP (human):(ki)14.4 pM
In vitro
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[2].?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[3].
In vivo
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[4].
AliasBIBN4096BS hydrochloride, BIBN-4096 hydrochloride
Chemical Properties
Molecular Weight906.11
FormulaC38H48Br2ClN9O5
Cas No.586368-06-1
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 66.66 mg/mL (73.57 mM)
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM1.1036 mL5.5181 mL11.0362 mL55.1809 mL
5 mM0.2207 mL1.1036 mL2.2072 mL11.0362 mL
10 mM0.1104 mL0.5518 mL1.1036 mL5.5181 mL
20 mM0.0552 mL0.2759 mL0.5518 mL2.7590 mL
50 mM0.0221 mL0.1104 mL0.2207 mL1.1036 mL

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