Necrostatin-1 (Nec-1) 是一种有效的能透过血脑屏障的坏死性凋亡 (necroptosis) 抑制剂,在 Jurkat 细胞中的EC50为 490 nM。Necrostatin-1 抑制RIP1激酶 (EC50=182 nM) 。Necrostatin-1 (Nec-1) 也是一种(IDO)抑制剂。
生物活性 | Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barriernecroptosis inhibitorwith anEC50of 490 nM in Jurkat cells. Necrostatin-1 inhibitsRIP1 kinase(EC50=182 nM). Necrostatin-1 is also anIDOinhibitor[1]. |
IC50& Target | EC50: 182 nM (RIP1 kinase)[1] |
体外研究 (In Vitro) | Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors[1]. Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)[2]. Necrostatin-1 (Nec-1) (30 μM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death[4].
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体内研究 (In Vivo) | Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period[2].
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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 |
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溶解性数据 | In Vitro: DMSO : ≥ 46 mg/mL(177.38 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 3.8561 mL | 19.2805 mL | 38.5609 mL | 5 mM | 0.7712 mL | 3.8561 mL | 7.7122 mL | 10 mM | 0.3856 mL | 1.9280 mL | 3.8561 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: 0.5%CMC-Na/saline water Solubility: 12.5 mg/mL (48.20 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% (50% EtOH 50% Cremophor EL) 90% saline Solubility: 1.67 mg/mL (6.44 mM); Suspended solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
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