PF-05231023

Alias: PF-5231023; PF5231023; PF 5231023; PF-05231023; PF05231023; PF 05231023;
Cat No.:V4561 Purity: ≥98%
PF-05231023 is novel and potent, long-actingFGF21-receptoragonist being developed as a potential treatment for T2DM.
PF-05231023 Chemical Structure CAS No.: 1037589-69-7
Product category: PROTAC Linkers
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PF-05231023 is novel and potent, long-acting FGF21-receptor agonist being developed as a potential treatment for T2DM. PF-05231023 is a FGF21 mimetic that decreases body weight and improves lipid profile in non-human primates and in type 2 diabetic subjects.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
The E3 ubiquitin ligase ligand and the target protein ligand are the two distinct ligands found in PROTAC, which are joined by a linker. Specifically, target proteins are degraded by PROTAC through the intracellular ubiquitin-proteasome system [1].
Animal Protocol
Animal/Disease Models: Eight week old Zucker rats[3]
Doses: 3 mg/kg and 10 mg/kg
Route of Administration: subcutaneously (sc) twice a week for two weeks
Experimental Results: 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/Disease Models: 7-to-8-month-old Akita mice with type 1 diabete model[4]
Doses: 10 mg/kg
Route of Administration: Intraperitoneally injected; twice a week; for four weeks
Experimental Results: Administration improved retinal function in diabetic Akita mice.
References
[1]. 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).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H32N4O8
Molecular Weight
528.554286956787
CAS #
1037589-69-7
SMILES
O=C(NCCOCCOCCC(NC1=CC=C(CCC(N2C(CC2)=O)=O)C=C1)=O)CCN3C(C=CC3=O)=O
InChi Key
BJDLYWUPKGDHCF-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H32N4O8/c31-21(9-13-29-24(34)7-8-25(29)35)27-12-16-38-18-17-37-15-11-22(32)28-20-4-1-19(2-5-20)3-6-23(33)30-14-10-26(30)36/h1-2,4-5,7-8H,3,6,9-18H2,(H,27,31)(H,28,32)
Chemical Name
2,5-Dihydro-2,5-dioxo-N-[2-[2-[3-oxo-3-[[4-[3-oxo-3-(2-oxo-1-azetidinyl)propyl]phenyl]amino]propoxy]ethoxy]ethyl]-1H-pyrrole-1-propanamide
Synonyms
PF-5231023; PF5231023; PF 5231023; PF-05231023; PF05231023; PF 05231023;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~189.20 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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