2. Metabolic Enzyme/Protease
  3. Ketohexokinase
  4. KHK-IN-1

KHK-IN-1 (化合物8) 是一种具有选择性和细胞膜渗透性的己酮糖激酶 (KHK) 抑制剂 (IC50=12 nM; F=34%)。KHK-IN-1 能抑制 HepG2 细胞裂解液中 F1P 的产生 (IC50=400 nM)。KHK-IN-1 具有研究糖尿病和肥胖症的潜力。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 KHK-IN-1 hydrochloride 通常具有更好的水溶性和稳定性。

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KHK-IN-1 Chemical Structure

KHK-IN-1 Chemical Structure

CAS No. : 1303469-70-6

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KHK-IN-1 的其他形式现货产品:

Other Forms of KHK-IN-1:

KHK-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity[1].

IC50 & Target

IC50=12 nM (KHK)[1].
体外研究
(In Vitro)

KHK-IN-1 stable in human and rat liver microsome preparations (88 and 72% remaining at 10 min) and do not significantly inhibit cytochrome P450s from human liver microsomes (1A2, 2C19, 2D6, 2C9, and 3A4)[1].
KHK-IN-1 (0-10 µM; incubate 30 min, then add to 15 mM fructose and incubate for another 3 h) inhibits production of F1P in HepG2 cell lysates with an IC50 value of 400 nM[1].

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

KHK-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 cells
Concentration: 0-10 µM
Incubation Time: Incubate 30 min, then add to 15 mM fructose and incubate for another 3 h
Result: Exhibited inhibition of F1P production in HepG2 cell lysates (IC50=400 nM).
体内研究
(In Vivo)

KHK-IN-1 (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats[1].

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

Animal Model: Male Sprague-Dawley rats (~250 g)[1].
Dosage: 10 mg/kg
Administration: Oral gavage; single
Result: Exhibited reasonable oral bioavailability in rats (F=34%; oral t1/2=4 h), but had a high volume of distribution (Vdss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).
分子量

422.55

Formula

C21H26N8S
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

KHK-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

KHK-IN-11303469-70-6KetohexokinaseKHKNIDDMHepG2 cellF1PdiabetesobesityInhibitorinhibitorinhibit

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