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PF-05231023

Cat. No. M10048
PF-05231023 Structure
Synonym:

PF05231023

Size Price Availability Quantity
5mg USD 110  USD110 In stock
10mg USD 210  USD210 In stock
25mg USD 420  USD420 In stock
50mg USD 750  USD750 In stock
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Quality Control & Documentation
Biological Activity

PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM. PF-05231023 suppresses oxidative-stress-induced inflammation in photoreceptors. PF-05231023 decreases the variability of retinal NRF2 levels and displays a trend (non-significant) towards increased NRF2 levels in Akita mice. PF-05231023 (10 mg/kg; i.p.) reduces retinal inflammation in diabetic mice.

Chemical Information
Molecular Weight 528.55
Formula C26H32N4O8
CAS Number 1037589-69-7
Solubility (25°C) DMSO 100 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] Malte Hasle Nielsen, et al. Am J Physiol Gastrointest Liver Physiol. Hepatoprotective effects of the long-acting fibroblast growth factor 21 analog PF-05231023 in the GAN diet-induced obese and biopsy-confirmed mouse model of nonalcoholic steatohepatitis

[2] Tod Turner, et al. PLoS One. FGF21 increases water intake, urine output and blood pressure in rats

[3] Zhongjie Fu, et al. Diabetes. Fibroblast Growth Factor 21 Protects Photoreceptor Function in Type 1 Diabetic Mice

[4] Junichiro Sonoda, et al. Horm Mol Biol Clin Investig. FGF21-receptor agonists: an emerging therapeutic class for obesity-related diseases

[5] Jennifer Q Dong, et al. Br J Clin Pharmacol. Pharmαcοkinetics and phαrmacodynamιcs of PF-05231023, a novel long-acting FGF21 mimetic, in a first-in-hυman study

[6] Craig Giragossian, et al. Drυg Metab Dispos. Mechanistic investigation of the preclinιcal pharmαcοkinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate

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