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.
| 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 |
| 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.
| Related CGRP Receptor Products |
|---|
| Rimegepant Sulfate
Rimegepant Sulfate is a potent, selective, competitive, orally active calcitonin gene-related peptide (CGRP) antagonist with a Ki of 0.027 nM.May be used in migraine-related studies. |
| Calcitonin (human)
Calcitonin (human) is a calcitonin that lowers blood calcium levels and inhibits bone resorption and may be used in studies related to hypercalcemia or osteoporosis. |
| Cagrilintide acetate
Cagrilintide acetate is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake. Cagrilintide has the potential for the research of obesity. |
| Vazegepant
Vazegepant is the first intranasal CGRP receptor antagonist for the study the acute research of migraine. |
| α-CGRP, human TFA
α-CGRP, human TFA is a regulatory neuropeptide of 37 amino acids. α-CGRP, human TFA can be used as a potent vasodilator. |
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