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PF-05231023

SKU: orb1219688

Description

PF-05231023 is a long-acting fibroblast growth factor 21 (FGF21) analog and is an FGF21-receptor agonist. It is also suitable for development as a potential treatment for T2DM. PF-05231023 is a analog of long-acting fibroblast growth factor 21.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 decreases retinal IL-1β mRNA expression in Akita mice. PF-05231023 enhances cone-specific arrestin4 expression in Akita mice. PF-05231023 restores photoreceptor morphology in Akita mice. Administration of native FGF21 and PF-05231023 (3 mg/kg or 10 mg/kg; subcutaneously twice a week for two weeks) improves glucose tolerance and liver insulin sensitivity in Zucker rats. PF-05231023 (10 mg/kg; intraperitoneally injected) reduces retinal inflammation in diabetic mice.(In Vivo):Animal Model: Eight week old Zucker ratsDosage: 3 mg/kg and 10 mg/kg.Administration: Subcutaneously twice a week for two weeks.Result: There was no change of BW observed, and food intake was not changed in the treated groups compared to control. Caused a significant decrease of glucose excursion during the oral glucose tolerance test (OGTT) compared to control.

Images & Validation

Key Properties

CAS Number1037589-69-7
MW528.55
Purity>98% (HPLC)
FormulaC26H32N4O8
SMILESO=C(CCN1C(=O)C=CC1=O)NCCOCCOCCC(=O)Nc1ccc(CCC(=O)N2CCC2=O)cc1
TargetFGF21-receptor
SolubilityDMSO:125 mg/mL (236.50 mM; Need ultrasonic)

Bioactivity

In Vivo
Animal model: Eight week old Zucker rats. Dosage: 3 mg/kg and 10 mg/kg. Administration: Subcutaneously twice a week for two weeks. Result: There was no change of BW observed, and food intake was not changed in the treated groups compared to control. Caused a significant decrease of glucose excursion during the oral glucose tolerance test (OGTT) compared to control. Animal model: 7-to-8-month-old Akita mice with type 1 diabete model. Dosage: 10 mg/kg. Administration: Intraperitoneally injected; twice a week; for four weeks. Result: Administration improved retinal function in diabetic Akita mice.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information

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