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PF-06291874

Cat. No. M8113
PF-06291874 Structure
Size Price Availability Quantity
10mM*1mL USD 423  USD470 In stock
2mg USD 279  USD310 In stock
5mg USD 387  USD430 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

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 503.51
Formula C26H28F3N3O4
CAS Number 1393124-08-7
Purity >98%
Solubility DMSO: 15 mg/mL
Storage at -20°C
References

Identification of a novel conformationally constrained glucagon receptor antagonist.
Lee EC, et al. Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. PMID: 24418771.

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.
Guzman-Perez A, et al. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. PMID: 23562063.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-06291874 supplier, Glucagon Receptor, inhibitors

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