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Olcegepant hydrochloride

Cat. No. M13934
Olcegepant hydrochloride Structure
Synonym:

BIBN-4096 hydrochloride; BIBN4096BS hydrochloride

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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 906.11
CAS Number 586368-06-1
Solubility (25°C) DMSO 90 mg/mL
Water ≥ 66.66 mg/mL
Storage 2-8°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Amna C Mazeh, et al. Cannabidiol selectively inhibits the contraction of rat small resistance arteries: Possible role for CGRP and voltage-gated calcium channels

[2] M Bayes, et al. Gateways to clinical trials

[3] M Bayes, et al. Gateways to clinical trials

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Keywords: Olcegepant hydrochloride, BIBN-4096 hydrochloride; BIBN4096BS hydrochloride supplier, CGRP Receptor, inhibitors, activators

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