2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. GNF2133 hydrochloride

GNF2133 hydrochloride 是一种有效的、选择性的、具有口服活性的 DYRK1A 抑制剂，对 DYRK1A 和 GSK3β 的 IC50 分别为 0.0062、>50 µM。GNF2133 hydrochloride 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 hydrochloride 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 hydrochloride 具有研究1型糖尿病的潜力。

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GNF2133 hydrochloride Chemical Structure

GNF2133 hydrochloride Chemical Structure

CAS No. : 2561414-57-9

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规格 价格 是否有货
1 mg ￥1600
询问价格 & 货期
5 mg ￥4000
询问价格 & 货期
10 mg ￥6000
询问价格 & 货期

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GNF2133 hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of GNF2133 hydrochloride:

GNF2133 hydrochloride 相关抗体

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查看 DYRK 亚型特异性产品:

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DYRK1 DYRK2 DYRK3 DYRK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes[1].

IC50 & Target[1]

DYRK1

 

DYRK1A

0.0062 μM (IC50)

GSK3β

>50 μM (IC50)

体内研究
(In Vivo)

GNF2133 hydrochloride (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3%[1].
GNF2133 hydrochloride (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].
GNF2133 hydrochloride (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].
Pharmacokinetic Parameters of GNF2133 hydrochloride in CD-1 mice[1].

plasma (iv) plasma (po) pancreas (po)
CL (mL/min/kg) 23.5 / /
Vss (L/kg) 11 / /
AUC (h·nM) 3268 10974 144420
Cmax(nM) 1977 1675 13319
tmax<(h) 0.03 3.0 3.0
Clast(nM) 36.6 19 1324
t1/2<(h) 6.6 3.4 6.6
F (%) / 22.3 /
CD-1 mice; 30 mg/kg; p.o.[1].

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

Animal Model: CD-1 mice[1]
Dosage: 30 mg/kg
Administration: P.o.
Result: Showed good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%.
Animal Model: Wistar Han rat[1]
Dosage: 30 mg/kg (0.5% methylcellulose + Tween-80)
Administration: P.o.; once a day for 5 days
Result: Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin.
Animal Model: Diphtheria toxin A (RIP-DTA) mice[1]
Dosage: 3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days)
Administration: P.o., once a day for 35 days
Result: Significantly improves glucose disposal capacity and increased insulin secretion.
分子量

470.99

Formula

C24H31ClN6O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GNF2133 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNF21332561414-57-9GNF 2133GNF-2133DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseorally activeβ-cellglucose disposalinsulin secretionCD-1 miceRIP-DTA miceInhibitorinhibitorinhibit

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