PF-04937319

Name: PF-04937319
Brand: TargetMol
SKU: T16479
Price: 363 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.89%

货号 T16479Cas号 1245603-92-2

PF-04937319 是一种葡萄糖激酶激活剂 (EC50 =154.4 μM)。 PF-04937319 保持降糖功效，同时降低许多其他 GKA 观察到的低血糖风险。 PF-04937319可用于治疗2型糖尿病的研究。

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PF-04937319

一键复制产品信息

很棒

纯度: 99.89%

货号 T16479Cas号 1245603-92-2

规格	价格	库存
1 mg	¥ 363	现货
5 mg	¥ 888	现货
10 mg	¥ 1,550	现货
25 mg	¥ 3,230	现货
50 mg	¥ 4,720	现货
100 mg	¥ 6,730	现货
1 mL x 10 mM (in DMSO)	¥ 866	现货

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COA LCMS HNMR 产品操作手册

产品介绍

PF-04937319 AI Summary

PF-04937319 is a multifaceted bioactive compound demonstrating diverse biological activities across several systems. It notably activates human recombinant glucokinase and promotes glucokinase translocation from the nucleus to the cytoplasm in rat hepatocytes. The compound shows enhanced drug uptake via human hepatic OATP1B1 and OATP1B3 transporters and possesses apparent permeability across dog RRCK cells. Its lipophilicity, with a LogD7.4 value of 2.1, suggests favorable bioavailability and interaction potential with lipid bilayers. In pharmacokinetic studies, PF-04937319 exhibits a high fraction unbound in rat plasma. It shows activation of glucokinase by increasing enzyme velocity and altering the glucokinase Km, with an EC50 of 190.0 nM in a glucose-present assay. The compound also demonstrates antidiabetic potential in Sprague-Dawley rats and exhibits a therapeutic index greater than 5.0. It has demonstrated antiviral activity against SARS-CoV-2, reducing cytotoxicity in Caco-2 and VERO-6 cells at a concentration of 10 μM, although with varying inhibitory percentages. Additionally, PF-04937319 shows inhibition of the SARS-CoV-2 3CL-Pro protease and exhibits minor inhibitory activity on human HDAC6. With its diverse bioactivities, particularly in glucose metabolism regulation, antiviral properties, and high permeability, PF-04937319 is a promising candidate for further pharmacological exploration..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	PF-04937319 is an activator of glucokinase (EC50 =154.4 μM). PF-04937319 maintains glucose-lowering efficacy while mitigating the risk of hypoglycemia observed with many other glucokinase activators. PF-04937319 can be used in research on the treatment of type 2 diabetes mellitus.
靶点活性	GK:154.4 μM(EC50)

化学信息

分子量	432.43
分子式	C₂₂H₂₀N₆O₄
CAS No.	1245603-92-2
Smiles	CN(C)C(=O)c1ncc(Oc2cc(cc3oc(C)cc23)C(=O)Nc2cnc(C)cn2)cn1
密度	1.366 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 95 mg/mL (219.69 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3125 mL	11.5626 mL	23.1251 mL	115.6257 mL
5 mM	0.4625 mL	2.3125 mL	4.6250 mL	23.1251 mL
10 mM	0.2313 mL	1.1563 mL	2.3125 mL	11.5626 mL
20 mM	0.1156 mL	0.5781 mL	1.1563 mL	5.7813 mL
50 mM	0.0463 mL	0.2313 mL	0.4625 mL	2.3125 mL
100 mM	0.0231 mL	0.1156 mL	0.2313 mL	1.1563 mL