PF-0637222 | CAS# | GCGR/GLP1 NAM

MedKoo Cat#: 571513 | Name: PF-06372222

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PF-06372222 is a small-molecule negative allosteric modulator (NAM) of glucagon receptor (GCGR). Antagonists of GCGR may be helpful in treating type 2 diabetes mellitus because they regulate plasma glucose levels by decreasing or slowing hepatic glucose production by signaling in the liver, intestinal smooth muscle, kidney, brain, and adipose tissue. PF-06372222 is also an antagonist for glucagon-like peptide-1 receptor GLP-1R, which inhibits glucagon secretion and glucose-dependent insulin secretion and may also play a role in hormonal release leading to acute and chronic stress and anxiety. By negatively modulating GLP-1R, PF-06372222 could treat type 2 diabetes mellitus and stress and anxiety.

Chemical Structure

PF-06372222

CAS#1407592-99-7

Theoretical Analysis

MedKoo Cat#: 571513

Name: PF-06372222

CAS#: 1407592-99-7

Chemical Formula: C26H28F3N5O3

Exact Mass: 515.2144

Molecular Weight: 515.54

Elemental Analysis: C, 60.57; H, 5.47; F, 11.06; N, 13.58; O, 9.31

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

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Synonym

PF-0637222; PF0637222; PF 0637222

IUPAC/Chemical Name

(R)-3-(4-((3,3-dimethylcyclobutyl)((6-(4-(trifluoromethyl)-1H-imidazol-1-yl)pyridin-3-yl)amino)methyl)benzamido)propanoic acid

InChi Key

MYZIDYJMNWEJMC-QHCPKHFHSA-N

InChi Code

InChI=1S/C26H28F3N5O3/c1-25(2)11-18(12-25)23(16-3-5-17(6-4-16)24(37)30-10-9-22(35)36)33-19-7-8-21(31-13-19)34-14-20(32-15-34)26(27,28)29/h3-8,13-15,18,23,33H,9-12H2,1-2H3,(H,30,37)(H,35,36)/t23-/m0/s1

SMILES Code

FC(F)(F)C1=CN(C2=CC=C(N[C@@H](C3=CC=C(C(NCCC(O)=O)=O)C=C3)C4CC(C)(C)C4)C=N2)C=N1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

G-protein-coupled receptors (GPCRs) are signal receptors encoded by approximately 1000 Genes. They are targets in therapies involving neurotransmitters, hormones, peptides, chemokines, lipids, purines, ions, photons, and odorants, and thus can be used in treating central nervous system disorders, cancers, and cardiac, metabolic, and inflammatory diseases.

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 515.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC. Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators. Nature. 2017 Jun 8;546(7657):312-315. doi: 10.1038/nature22378. Epub 2017 May 17. PubMed PMID: 28514449. 2: Lu S, Zhang J. Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug-Target Interactions. J Med Chem. 2018 Feb 26. doi: 10.1021/acs.jmedchem.7b01844. [Epub ahead of print] PubMed PMID: 29457894.