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KU-32 Sale

目录号 : GC31118

KU-32是一种新型的,基于新生霉素的Hsp90抑制剂,可以预防神经细胞死亡。

KU-32 Chemical Structure

Cas No.:956498-70-7

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Sample solution is provided at 25 µL, 10mM.

Description

KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.

Treating human islets with KU-32 for 24 hours shows no toxicity. With a minimum of 2-day exposure, KU-32 improves cellular viability by blocking apoptosis. Functionally, isolated human islets release more glucose-stimulated insulin when preincubate in KU-32[1]. KU-32 protects against glucose-induced death of embryonic DRG (dorsal root ganglia) neurons cultured for 3 days in vitro[2].

Diabetic BKS-db/db mice, a model for type 2 diabetes, administered KU-32 for 10 weeks do not show any significant changes in blood glucose and insulin levels, despite having greater insulin staining/beta cell in the pancreas compared to untreated BKS db/db mice[1].

[1]. Farmer K, et al. KU-32, a novel drug for diabetic neuropathy, is safe for human islets and improves in vitro insulin secretion and viability. Exp Diabetes Res. 2012;2012:671673. [2]. Urban MJ, et al. Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice. ASN Neuro. 2010 Aug 11;2(4):e00040.

实验参考方法

Cell experiment:

Islets are placed into 96-well plates and subjected to a 8-point dose of KU-32 in either low (5 mM) or high (17.5 mM) glucose in DMEM : F12 media and incubated overnight at 37°C and 5% CO2. Twenty-four hours later, alamarBlue is added directly to each well to achieve a final concentration of 10% alamarBlue. Readings on a microplate reader are collected 4, 24, and 48 hours later[1].

Animal experiment:

Male and female lepr mice are used. At 10 weeks of age, animals are given once per week intraperitoneal injection of 5% Captisol or 20 mg/kg KU-32 in 5% Captisol. At termination of the study, blood from each animal is collected[1].

References:

[1]. Farmer K, et al. KU-32, a novel drug for diabetic neuropathy, is safe for human islets and improves in vitro insulin secretion and viability. Exp Diabetes Res. 2012;2012:671673.
[2]. Urban MJ, et al. Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice. ASN Neuro. 2010 Aug 11;2(4):e00040.

化学性质

Cas No. 956498-70-7 SDF
Canonical SMILES CC1=C(O2)C(C=C(NC(C)=O)C2=O)=CC=C1O[C@H]3[C@@H]([C@@H]([C@@H](OC)C(C)(C)O3)O)O
分子式 C20H25NO8 分子量 407.41
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4545 mL 12.2726 mL 24.5453 mL
5 mM 0.4909 mL 2.4545 mL 4.9091 mL
10 mM 0.2455 mL 1.2273 mL 2.4545 mL
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