GNF4877|cas:2041073-22-5|西域试剂

GNF4877,98.85%

产品编号：Bellancom-129492| CAS NO：2041073-22-5| 分子式：C₂₅H₂₇FN₆O₄| 分子量：494.52

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货号	价格	库存与货期
Bellancom-129492	￥2350.00	杭州北京（现货）
Bellancom-129492	￥7000.00	杭州北京（现货）
Bellancom-129492	￥11000.00	杭州北京（现货）
Bellancom-129492	￥0.00	杭州北京（现货）
Bellancom-129492	￥0.00	杭州北京（现货）

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GNF4877

产品介绍

GNF4877是 DYRK1A 和 GSK3β 的有效抑制剂，IC₅₀ 值分别为 6 nM 和 16 nM，可导致 NFATc 核输出受阻并增加 β 细胞增殖 (对小鼠 β (R7T1) 细胞的 EC₅₀ 值为 0.66 μM)。

生物活性

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).

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)
Dosage:	50 mg/kg
Administration:	Oral gavage; twice a day; for 15 days
Result:	Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)
Dosage:	50 mg/kg
Administration:	Oral gavage; twice a day; for 15 days
Result:	Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.

性状

Solid

溶解性数据

In Vitro:

DMSO : 4.17 mg/mL (8.43 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	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	---	---	---

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式