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MK-2894

Cat. No. M10858
MK-2894  Structure
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MK-2894 IS AN EFFECTIVE, SELECTIVE, HIGH-AFFINITY (Ki=0.56 nM) of prostaglandin receptor 4 (EP4 receptor) antagonists (IC50=2.5 nM)。 MK-2894 has strong anti-inflammatory activity in animal pain/inflammation models and can be used in arthritis studies.

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 473.51
Formula C25H22F3NO3S
CAS Number 1006036-87-8
Purity >98%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
References

[1] Marc Blouin, et al. J Med Chem. The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist

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Keywords: MK-2894 supplier, Prostaglandin Receptor, inhibitors

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