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Vazegepant (BHV-3500) hydrochloride is a highly affinity CGRP receptor antagonist (hCGRP Ki= 0.023 nM). Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation.
| 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.
| Molecular Weight | 675.26 |
| Formula | C36H47ClN8O3 |
| CAS Number | 1414976-20-7 |
| Purity | >98% |
| Solubility | Water 50 mg/mL DMSO 50 mg/mL |
| Storage | at -20°C |
| Related CGRP Receptor Products |
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| Ubrogepant
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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. |
| Rimegepant
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)
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
BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM. |
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