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MK-0974

Cat. No. M3618
MK-0974 Structure
Synonym:

Telcagepant

Size Price Availability
10mg USD 465  USD465 Out of stock
50mg USD 1350  USD1350 Out of stock
100mg USD 2100  USD2100 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 566.52
Formula C26H27F5N6O3
CAS Number 781649-09-0
Purity >98%
Solubility DMSO
Storage at -20°C
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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Keywords: MK-0974, Telcagepant supplier, CGRP Receptor, inhibitors

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