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MedKoo CAT#: 530533
CAS#: 1037589-69-7
Description: PF-05231023 is a long-acting FGF21 mimetic. PF-05231023 decreases body weight and improves lipid profile in non-human primates and in type 2 diabetic subjects.
MedKoo Cat#: 530533
Name: PF-05231023
CAS#: 1037589-69-7
Chemical Formula: C26H32N4O8
Exact Mass: 528.222
Molecular Weight: 528.56
Elemental Analysis: C, 59.08; H, 6.10; N, 10.60; O, 24.22
Synonym: PF-05231023; PF05231023; PF 05231023; PF-5231023; PF5231023; PF 5231023
IUPAC/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
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)
SMILES Code: O=C(NCCOCCOCCC(NC1=CC=C(CCC(N2C(CC2)=O)=O)C=C1)=O)CCN3C(C=CC3=O)=O
1: Talukdar S, Zhou Y, Li D, Rossulek M, Dong J, Somayaji V, Weng Y, Clark R, Lanba A, Owen BM, Brenner MB, Trimmer JK, Gropp KE, Chabot JR, Erion DM, Rolph TP, Goodwin B, Calle RA. A Long-Acting FGF21 Molecule, PF-05231023, Decreases Body Weight and Improves Lipid Profile in Non-human Primates and Type 2 Diabetic Subjects. Cell Metab. 2016 Mar 8;23(3):427-40. doi: 10.1016/j.cmet.2016.02.001. PubMed PMID: 26959184.
2: Dong JQ, Rossulek M, Somayaji VR, Baltrukonis D, Liang Y, Hudson K, Hernandez-Illas M, Calle RA. 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. doi: 10.1111/bcp.12676. PubMed PMID: 25940675; PubMed Central PMCID: PMC4631178.
3: Giragossian C, Vage C, Li J, Pelletier K, Piché-Nicholas N, Rajadhyaksha M, Liras J, Logan A, Calle RA, Weng Y. 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. doi: 10.1124/dmd.114.061713. PubMed PMID: 25805881.
4: Weng Y, Chabot JR, Bernardo B, Yan Q, Zhu Y, Brenner MB, Vage C, Logan A, Calle R, Talukdar S. Pharmacokinetics (PK), pharmacodynamics (PD) and integrated PK/PD modeling of a novel long acting FGF21 clinical candidate PF-05231023 in diet-induced obese and leptin-deficient obese mice. PLoS One. 2015 Mar 19;10(3):e0119104. doi: 10.1371/journal.pone.0119104. PubMed PMID: 25790234; PubMed Central PMCID: PMC4366384.
5: Thompson WC, Zhou Y, Talukdar S, Musante CJ. PF-05231023, a long-acting FGF21 analogue, decreases body weight by reduction of food intake in non-human primates. J Pharmacokinet Pharmacodyn. 2016 Aug;43(4):411-25. doi: 10.1007/s10928-016-9481-1. PubMed PMID: 27405817; PubMed Central PMCID: PMC4954843.
6: Bernardo B, Lu M, Bandyopadhyay G, Li P, Zhou Y, Huang J, Levin N, Tomas EM, Calle RA, Erion DM, Rolph TP, Brenner M, Talukdar S. 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. doi: 10.1038/srep11382. PubMed PMID: 26153793; PubMed Central PMCID: PMC4495598.
