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Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $107 | Backorder |
Description | Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM. |
Targets&IC50 | CGRP:0.03 nM |
In vitro | Olcegepant hydrochloride shows high binding affinity to human CGRP receptors (IC₅₀ = 0.03 nM) and pure antagonist behavior (pA₂ = 11.1) in SK-N-MC cells[1]. |
In vivo | In Wistar rats, Olcegepant hydrochloride (900 μg/kg, i.v.) reduced capsaicin-induced Fos expression in the spinal trigeminal nucleus by 57%, with no effect on trigeminal ganglion pERK, indicating a central site of CGRP receptor inhibition[4]. |
Alias | BIBN4096BS hydrochloride, BIBN-4096 hydrochloride, BIBN4096 hydrochloride, BIBN 4096BS hydrochloride |
Molecular Weight | 906.11 |
Formula | C38H48Br2ClN9O5 |
Cas No. | 586368-06-1 |
Smiles | O=C1N(CC=2C(N1)=CC=CC2)C3CCN(C(N[C@H](CC4=CC(Br)=C(O)C(Br)=C4)C(N[C@H](C(=O)N5CCN(CC5)C=6C=CN=CC6)CCCCN)=O)=O)CC3.Cl |
Relative Density. | 1.31g/cm3 |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice./Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (88.29 mM), Sonication is recommended. H2O: 50 mg/mL (55.18 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
H2O/DMSO
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