BGP-15 - CAS:66611-37-8

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BGP-15

目录号 : KM7459 CAS No. : 66611-37-8 纯度 : ≥98%

Data Sheet 产品使用指南

BGP-15 是一种 PARP 抑制剂，IC₅₀ 和 K_i 值分别为 120 和 57 μM。

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10mg		In-stock
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200mg	询价	In-stock

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生物活性

BGP-15 is a PARP inhibitor, with an IC₅₀ and a K_i of 120 and 57 μM, respectively.

体外研究

BGP-15 (200 μM) prevents the imatinib mesylate-induced oxidative damages, attenuates the depletion of high-energy phosphates, alters the signaling effect of imatinib mesylate by preventing p38 MAP kinase and JNK activation, and induced the phosphorylation of Akt and GSK-3beta.

体内研究

BGP-15 (15 mg/kg, p.o.) does not improve skeletal muscle pathology in older mdx mice. In a rat model, 10 days of BGP-15 treatment greatly improves diaphragm muscle fiber function (by about 100%), although it does not reverse diaphragm atrophy. The treatment also provides protection from myosin PTMs associated with HSP72 induction and PARP-1 inhibition, resulting in improvement of mitochondrial function and content. BGP-15 (15 mg/kg per day in saline) treatment has no effect in Ntg mice or an independent cohort of normal adult wild-type mice based on morphology, cardiac function and ECG parameters. Treatment with BGP-15 attenuates the increase in atrial size and lung weight. BGP-15 treatment is able to prevent or reduce episodes of arrhythmia. BGP-15 treatment is associated with a reduced PR interval in the HF+AF model. BGP-15 (10 and 30 mg/kg) increases insulin sensitivity by 50% and 70%, respectively, in cholesterol-fed but not in normal rabbits. After 5 days of treatment with BGP-15, the glucose infusion rate is increased in a dose-dependent manner in genetically insulin-resistant GK rats. The most effective dose is 20 mg/kg, which shows a 71% increase in insulin sensitivity compared to control group.

分子式

C₁₄H₂₄Cl₂N₄O₂

分子量

351.27

CAS号

66611-37-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : 100 mg/mL (284.68 mM; Need ultrasonic)

DMSO : 11.33 mg/mL (32.25 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8468 mL	14.2341 mL	28.4681 mL
5 mM	0.5694 mL	2.8468 mL	5.6936 mL
10 mM	0.2847 mL	1.4234 mL	2.8468 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。-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: ≥ 2.5 mg/mL (7.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。