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MK-3207 hydrochloride

Cat. No. M2133
MK-3207 hydrochloride Structure
Size Price Availability Quantity
10mg USD 275  USD275 In stock
50mg USD 820  USD820 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MK-3207 hydrochloride is a potent and orally bioavailable calcitonin gene-related peptide (CGRP) receptor antagonist. MK-3207 potently inhibits human α-CGRP-induced cAMP production in HEK293 cells stably expressing human CLR/RAMP1 with an IC50 of 0.12 nM, and maintains similar potency in the presence of 50% human serum with an IC50 of 0.17 nM, indicating that the activity of MK-3207 would not be dramatically affected by plasma protein binding in vivo. MK-3207 displays lower affinity for CGRP receptors from other species, including canine and rodent. MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. In vitro, MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM).

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 594.05
Formula C31H29F2N5O3.HCl
CAS Number 957116-20-0
Purity >98%
Solubility DMSO 110 mg/mL
Ethanol 110 mg/mL
Storage at -20°C
References

[1] Hewitt DJ, et al. Cephalalgia. Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine.

[2] Salvatore CA, et al. J Pharmacol Exp Ther. Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.

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