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MK-0974

Cat. No. M3618
MK-0974 Structure
Synonym:

Telcagepant

Size Price Availability
10mg USD 370  USD370 Out of stock
50mg USD 1200  USD1200 Out of stock
100mg USD 1920  USD1920 Out of stock
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Quality Control & Documentation
Biological Activity

MK-0974 (Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively. MK-0974 displays >1500-fold lower affinity for the canine and rat receptors. MK-0974 displays reversible and saturable binding to both SK-N-MC membranes and rhesus cerebellum with a K(D) of 1.9 nM and 1.3 nM, respectively.

Chemical Information
Molecular Weight 566.52
Formula C26H27F5N6O3
CAS Number 781649-09-0
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Moore EL, et al. Eur J Pharmacol. Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment of migraine.

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