KHK-IN-1 hydrochloride|cas:1303470-48-5|西域试剂

KHK-IN-1 hydrochloride,98.47%

产品编号：Bellancom-12841A| CAS NO：1303470-48-5| 分子式：C₂₁H₂₇ClN₈S| 分子量：459.01

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货号	价格	库存与货期
Bellancom-12841A	￥3500.00	杭州北京（现货）
Bellancom-12841A	￥6000.00	杭州北京（现货）
Bellancom-12841A	￥18000.00	杭州北京（现货）

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KHK-IN-1 hydrochloride

产品介绍

KHK-IN-1 hydrochloride (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 hydrochloride 能抑制 HepG2 细胞裂解液中 F1P 的产生 (IC₅₀=400 nM)。KHK-IN-1 hydrochloride 具有研究糖尿病和肥胖症的潜力。

生物活性

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

体外研究

KHK-IN-1 hydrochloride 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).
KHK-IN-1 hydrochloride (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.

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

Cell Viability Assay

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 hydrochloride (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats.

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

Animal Model:	Male Sprague-Dawley rats (~250 g).
Dosage:	10 mg/kg
Administration:	Oral gavage; single
Result:	Exhibited reasonable oral bioavailability in rats (F=34%; oral t_1/2=4 h), but had a high volume of distribution (Vd_ss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).

体内研究

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

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

Animal Model:	Male Sprague-Dawley rats (~250 g).
Dosage:	10 mg/kg
Administration:	Oral gavage; single
Result:	Exhibited reasonable oral bioavailability in rats (F=34%; oral t_1/2=4 h), but had a high volume of distribution (Vd_ss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).

体内研究

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

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

Animal Model:	Male Sprague-Dawley rats (~250 g).
Dosage:	10 mg/kg
Administration:	Oral gavage; single
Result:	Exhibited reasonable oral bioavailability in rats (F=34%; oral t_1/2=4 h), but had a high volume of distribution (Vd_ss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (54.47 mM; Need ultrasonic)

H₂O : 14.29 mg/mL (31.13 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1786 mL	10.8930 mL	21.7860 mL
5 mM	0.4357 mL	2.1786 mL	4.3572 mL
10 mM	0.2179 mL	1.0893 mL	2.1786 mL

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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明