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MedKoo Cat#: 522488 | Name: PF-04937319
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Description:

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

PF-04937319 is a glucokinase activator which is under development for the treatment of type 2 diametes mellitus. Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primarily through its regulatory actions in pancreatic β-cells and liver hepatocytes. Conversion of glucose to glucose-6-phosphate by GK promotes glycogen synthesis in liver hepatocytes, and insulin release in the pancreatic β-cells.

Chemical Structure

PF-04937319
CAS#1245603-92-2

Theoretical Analysis

MedKoo Cat#: 522488

Name: PF-04937319

CAS#: 1245603-92-2

Chemical Formula: C22H20N6O4

Exact Mass: 432.1546

Molecular Weight: 432.44

Elemental Analysis: C, 61.10; H, 4.66; N, 19.43; O, 14.80

Price and Availability

Size Price Availability Quantity
5mg USD 400.00 2 Weeks
25mg USD 800.00 2 Weeks
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Related CAS #
No Data
Synonym
PF-04937319; PF04937319; PF 04937319; PF-4937319; PF 4937319; PF4937319, nerigliatin
IUPAC/Chemical Name
N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide
InChi Key
MASKQITXHVYVFL-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H20N6O4/c1-12-8-24-19(11-23-12)27-21(29)14-6-17-16(5-13(2)31-17)18(7-14)32-15-9-25-20(26-10-15)22(30)28(3)4/h5-11H,1-4H3,(H,24,27,29)
SMILES Code
O=C(C1=NC=C(OC2=C3C=C(C)OC3=CC(C(NC4=NC=C(C)N=C4)=O)=C2)C=N1)N(C)C
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, not in water
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4  μM.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMSO 100.0 231.25
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 432.44 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.

Recalculate based on batch purity %
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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Kamimura H, Uehara S, Yoneda N, Suemizu H. Empirical scaling factor for predicting human pharmacokinetic profiles of disproportionate metabolites using the Css-MRTpo method and chimeric mice with humanised livers. Xenobiotica. 2023 Dec;53(8-9):523-535. doi: 10.1080/00498254.2023.2280785. Epub 2023 Nov 26. PMID: 37938160. 2: Kamimura H, Uehara S, Suemizu H. A novel Css-MRTpo approach to simulate oral plasma concentration-time profiles of the partial glucokinase activator PF-04937319 and its disproportionate N-demethylated metabolite in humans using chimeric mice with humanized livers. Xenobiotica. 2020 Jul;50(7):761-768. doi: 10.1080/00498254.2019.1693082. Epub 2019 Nov 22. PMID: 31721621. 3: Dzyurkevich MS, Babkov DA, Shtyrlin NV, Mayka OY, Iksanova AG, Vassiliev PM, Balakin KV, Spasov AA, Tarasov VV, Barreto G, Shtyrlin YG, Aliev G. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci Rep. 2017 Nov 22;7(1):16072. doi: 10.1038/s41598-017-16405-2. Erratum in: Sci Rep. 2018 Apr 19;8(1):6489. doi: 10.1038/s41598-018-24838-6. PMID: 29167582; PMCID: PMC5700121. 4: Denney WS, Denham DS, Riggs MR, Amin NB. Glycemic Effect and Safety of a Systemic, Partial Glucokinase Activator, PF-04937319, in Patients With Type 2 Diabetes Mellitus Inadequately Controlled on Metformin-A Randomized, Crossover, Active-Controlled Study. Clin Pharmacol Drug Dev. 2016 Nov;5(6):517-527. doi: 10.1002/cpdd.261. Epub 2016 May 6. PMID: 27870481. 5: Kamimura H, Ito S, Chijiwa H, Okuzono T, Ishiguro T, Yamamoto Y, Nishinoaki S, Ninomiya SI, Mitsui M, Kalgutkar AS, Yamazaki H, Suemizu H. Simulation of human plasma concentration-time profiles of the partial glucokinase activator PF-04937319 and its disproportionate N-demethylated metabolite using humanized chimeric mice and semi-physiological pharmacokinetic modeling. Xenobiotica. 2017 May;47(5):382-393. doi: 10.1080/00498254.2016.1199063. Epub 2016 Jul 7. PMID: 27389028. 6: Amin NB, Aggarwal N, Pall D, Paragh G, Denney WS, Le V, Riggs M, Calle RA. Two dose-ranging studies with PF-04937319, a systemic partial activator of glucokinase, as add-on therapy to metformin in adults with type 2 diabetes. Diabetes Obes Metab. 2015 Aug;17(8):751-9. doi: 10.1111/dom.12474. Epub 2015 May 11. PMID: 25885172. 7: Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, Pettersen JC, Goosen TC, Di L, Lee E, Pfefferkorn JA, Dalvie DK, Kalgutkar AS. Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator. Drug Metab Dispos. 2014 Nov;42(11):1926-39. doi: 10.1124/dmd.114.060087. Epub 2014 Aug 20. PMID: 25142735. 8: Pettersen JC, Litchfield J, Neef N, Schmidt SP, Shirai N, Walters KM, Enerson BE, Chatman LA, Pfefferkorn JA. The relationship of glucokinase activator- induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies. Toxicol Pathol. 2014 Jun;42(4):696-708. doi: 10.1177/0192623314526006. Epub 2014 Apr 24. PMID: 24771080.

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