| 规格: | 98% |
| 分子量: | 407.41 |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
Background:
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.
Protocol:
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]. |
参考文献: [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. | |
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