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PF-06291874

Cat. No. M8113
PF-06291874 Structure
Size Price Availability Quantity
10mM*1mL USD 470  USD470 In stock
2mg USD 310  USD310 In stock
5mg USD 430  USD430 In stock
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Quality Control & Documentation
Biological Activity

PF-06291874 is an orally active, potent and selective glucagon receptor antagonist. PF-06291874 exhibits a robust glucose reductions in subjects with type 2 diabetes mellitus.

Chemical Information
Molecular Weight 503.51
Formula C26H28F3N3O4
CAS Number 1393124-08-7
Solubility (25°C) DMSO: 15 mg/mL
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] Lee EC, et al. Bioorg Med Chem Lett. Identification of a novel conformationally constrained glucagon receptor antagonist.

[2] Guzman-Perez A, et al. Bioorg Med Chem Lett. The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.

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Keywords: PF-06291874 supplier, Glucagon Receptor, inhibitors, activators


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