P-1075|cas:60559-98-0|西域试剂

P-1075,98.03%

产品编号：Bellancom-108573| CAS NO：60559-98-0| 分子式：C₁₂H₁₇N₅| 分子量：231.30

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-108573	￥2000.00	杭州北京（现货）
Bellancom-108573	￥3200.00	杭州北京（现货）
Bellancom-108573	￥5200.00	杭州北京（现货）

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P-1075

产品介绍

P-1075 是有效的、磺酰脲受体2相关的 ATP 敏感性的钾通道 (SUR2-K_IR6) 的激活剂，EC₅₀ 值为 45 nM。P-1075 还能在兔子中通过打开线粒体 K (ATP) 通道，产生活性氧，保护心脏。

生物活性

P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-K_IR6), with an EC₅₀ value of 45 nM for SUR2B-K_IR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.

体外研究

P1075 (3 nM) induces monophasic inhibition curves by competition-binding experiments, in the presence of MgATP.
P1075 (100 µM; 10 min) leads to rabbit cardiomyocytes to produce ROS in a K_ATP-dependent fashion.
P1075 (150 nM) reduces infarct size in isolated rabbit hearts compared to control animals (10.6% of the area at risk vs. 31.5%, P < 0.05).

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

Cell Viability Assay

Cell Line:	COS-7 cells
Concentration:	3-15 nM
Incubation Time:
Result:	Showed IC₅₀ value of 15 nM and Hill coefficient of 1.0.

Cell Viability Assay

Cell Line:	Adult rabbit cardiomyocytes
Concentration:	100 µM
Incubation Time:	10 min
Result:	Led to a 44% increase in ROS generation (P<0.001 vs. untreated cells).

体内研究
(In Vivo)

P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model.

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

Animal Model:	Male Sprague-Dawley rats subjected to 30 minutes of ischemia and 2 hours of reperfusion
Dosage:	1μg/kg
Administration:	Intravenous injection; 1μg/kg; once
Result:	Reduced infarct size (41.8%) compared to the vehicle.

体内研究

P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model.

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

Animal Model:	Male Sprague-Dawley rats subjected to 30 minutes of ischemia and 2 hours of reperfusion
Dosage:	1μg/kg
Administration:	Intravenous injection; 1μg/kg; once
Result:	Reduced infarct size (41.8%) compared to the vehicle.

体内研究

P1075 (intravenous injection; 1μg/kg; once) treatment shows the reduction of infarct size in ischemia model.

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

Animal Model:	Male Sprague-Dawley rats subjected to 30 minutes of ischemia and 2 hours of reperfusion
Dosage:	1μg/kg
Administration:	Intravenous injection; 1μg/kg; once
Result:	Reduced infarct size (41.8%) compared to the vehicle.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (1080.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.3234 mL	21.6169 mL	43.2339 mL
5 mM	0.8647 mL	4.3234 mL	8.6468 mL
10 mM	0.4323 mL	2.1617 mL	4.3234 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: ≥ 2.08 mg/mL (8.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.99 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 (8.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.99 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.99 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。