BIBN 4096 (Olcegepant) is a potent and selective CGRP receptor antagonist (IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively). Displays high affinity for human CGRP receptors (Ki = 14.4 pM); exhibits no significant affinity for 75 other receptors.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 45 mg/mL|
 Benoit Michot, et al. Pain . 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
|Related CGRP Receptor Products|
HTL22562 is a CGRP antagonist intended for use in studies of acute migraine.
Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
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.
MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.