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Pack Size | Price | Availability | Quantity |
---|---|---|---|
50 mg | $813 | Backorder |
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). |
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]. |
Alias | BIBN-4096 hydrochloride, BIBN4096BS hydrochloride |
Molecular Weight | 906.11 |
Formula | C38H48Br2ClN9O5 |
Cas No. | 586368-06-1 |
Storage | Powder: -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
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