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GNF4877

カタログ番号GC38787

GNF4877は、それぞれ6 nMと16 nMのIC50を持つ強力なDYRK1AおよびGSK3β阻害剤であり、活性化T細胞の核因子(NFATc)核外輸送の遮断とβ細胞増殖の増加をもたらします(マウスβのEC50は0.66 μM) (R7T1) 細胞)。

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GNF4877 化学構造

Cas No.: 2041073-22-5

サイズ 価格 在庫数 個数
1mg
$218.00
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5mg
$649.00
在庫あり
10mg
$1,020.00
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25mg
$1,947.00
在庫あり
50mg
$3,309.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of GNF4877

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells)[1].

High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signalling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) show additive activity with GNF4877[1].

GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control[1]. Animal Model: Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4 g; 82±2 days)[1]

[1]. Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372.

Chemical Properties of GNF4877

Cas No. 2041073-22-5 SDF
Canonical SMILES O=C([C@H]1CN(C2=C(NC(C3=NC(C4=CC(OC(C)C)=CC=C4F)=CN=C3N)=O)C=NC=C2)CCC1)O
Formula C25H27FN6O4 M.Wt 494.52
溶解度 DMSO: 4.17 mg/mL (8.43 mM and warming) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of GNF4877

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1 mg 5 mg 10 mg
1 mM 2.0222 mL 10.1108 mL 20.2216 mL
5 mM 0.4044 mL 2.0222 mL 4.0443 mL
10 mM 0.2022 mL 1.0111 mL 2.0222 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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