1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. PF-05231023

PF-05231023 

Cat. No.: HY-113697 Purity: 99.78%
Handling Instructions

PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM.

For research use only. We do not sell to patients.

PF-05231023 Chemical Structure

PF-05231023 Chemical Structure

CAS No. : 1037589-69-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 116 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 380 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM[1][5].

IC50 & Target

FGF21-receptor[5].

In Vitro

PF-05231023 is a long-acting fibroblast growth factor 21 (FGF21) analog[2].

In Vivo

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[3].
PF-05231023 (10 mg/kg; intraperitoneally injected) decreases retinal inflammation in diabetic mice. PF-05231023 reduces retinal IL-1β mRNA expression in Akita mice. PF-05231023 increases cone-specific arrestin4 expression in Akita mice. PF-05231023 restores photoreceptor morphology in Akita mice. PF-05231023 inhibits oxidative-stress-induced inflammation in photoreceptors. PF-05231023 decreases the variability of retinal NRF2 levels and shows a trend (non-significant) towards increased NRF2 levels in Akita mice[4].

Animal Model: Eight week old Zucker rats[3]
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[4]
Dosage: 10 mg/kg
Administration: Intraperitoneally injected; twice a week; for four weeks
Result: Administration improved retinal function in diabetic Akita mice.
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (236.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8920 mL 9.4598 mL 18.9197 mL
5 mM 0.3784 mL 1.8920 mL 3.7839 mL
10 mM 0.1892 mL 0.9460 mL 1.8920 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

528.55

Formula

C₂₆H₃₂N₄O₈

CAS No.

1037589-69-7

SMILES

O=C(CCN1C(C=CC1=O)=O)NCCOCCOCCC(NC2=CC=C(C=C2)CCC(N3C(CC3)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-05231023
Cat. No.:
HY-113697
Quantity:

PF-05231023

Cat. No.: HY-113697