Ubrogepant (MK-1602) is a novel oral calcitonin gene-associated peptide receptor (CGRP) antagonist with the potential to be used in acute migraine studies.
|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 ≥ 200 mg/mL|
|Related CGRP Receptor Products|
Calcitonin salmon is a calcium-regulating hormone that is a dual agonist of amylin and calcitonin receptors that stimulate bone production and inhibit bone resorption.
Vazegepant (BHV-3500) hydrochloride is a highly affinity CGRP receptor antagonist (hCGRP Ki= 0.023 nM).
Rimegepant, also known as BMS-927711, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist with a Ki value of 0.027 nM.
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide (CGRP) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
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