PF-05231023 (Synonyms: Mal-PEG2-AZD) |
| Catalog No.GC31495 |
PF-05231023 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1037589-69-7
Sample solution is provided at 25 µL, 10mM.
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].
PF-05231023 is a long-acting fibroblast growth factor 21 (FGF21) analog[2].
Administration of native FGF21 and PF-05231023 ( 3 mg/kg or 10 mg/kg ) improves glucose tolerance and liver insulin sensitivity in Zucker rats[3].PF-05231023 (10 mg/kg) shows protective effects on Akita retinas. PF-05231023 (10 mg/kg) decreases retinal inflammation in diabetic mice. PF-05231023 (10 mg/kg) administration reduces retinal IL-1β mRNA expression in Akita mice. PF-05231023 (10 mg/kg) administration increases cone-specific arrestin4 expression in Akita mice. PF-05231023 (10 mg/kg) administration restores photoreceptor morphology in Akita mice. PF-05231023 (10 mg/kg) inhibits oxidative-stress-induced inflammation in photoreceptors. PF-05231023 (10 mg/kg) administration decreases the variability of retinal NRF2 levels and shows a trend (non-significant) towards increased NRF2 levels in Akita mice[4].
References:
[1]. Dong JQ, et al. Pharmacokinetics and pharmacodynamics of PF-05231023, a novel long-acting FGF21 mimetic, in a first-in-human study. Br J Clin Pharmacol. 2015 Nov;80(5):1051-63.
[2]. Giragossian C, et al. Mechanistic investigation of the preclinical pharmacokinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate. Drug Metab Dispos. 2015 Jun;43(6):803-11.
[3]. Bernardo B, et al. FGF21 does not require interscapular brown adipose tissue and improves liver metabolic profile in animal models of obesity and insulin-resistance. Sci Rep. 2015 Jul 8;5:11382.
[4]. Fu Z, et al. Fibroblast Growth Factor 21 Protects Photoreceptor Function in Type 1 Diabetic Mice. Diabetes. 2018 May;67(5):974-985.
[5]. Sonoda J, et al. FGF21-receptor agonists: an emerging therapeutic class for obesity-related diseases. Horm Mol Biol Clin Investig. 2017 May 19;30(2).
| Cas No. | 1037589-69-7 | SDF | |
| Synonyms | Mal-PEG2-AZD | ||
| Canonical SMILES | O=C(CCN1C(C=CC1=O)=O)NCCOCCOCCC(NC2=CC=C(C=C2)CCC(N3C(CC3)=O)=O)=O | ||
| Formula | C26H32N4O8 | M.Wt | 528.55 |
| Solubility | DMSO : 125 mg/mL (236.50 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.892 mL | 9.4598 mL | 18.9197 mL |
| 5 mM | 0.3784 mL | 1.892 mL | 3.7839 mL |
| 10 mM | 0.1892 mL | 0.946 mL | 1.892 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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