Tranylcypromine hydrochloride (SKF 385 hydrochloride) 是 lysine-specific demethylase 1(LSD1/BHC110)和 monoamine oxidase(MAO)的不可逆抑制剂。Tranylcypromine hydrochloride 抑制 LSD1,MAO A 和 MAO B 的IC50值分别为 20.7,2.3 和 0.95 μM。Tranylcypromine hydrochloride 可用于忧郁症的研究。
生物活性 | Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1(LSD1/BHC110)andmonoamine oxidase(MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B withIC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression[1][2][3]. |
IC50& Target | MAO-A 2.3 μM (IC50) | MAO-B 0.95 μM (IC50) |
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体外研究 (In Vitro) | Tranylcypromine hydrochlorid (50 μM-5 mM; 1 h or 12-14 h) inhibits histone and nucleosomal demethylation[1].Tranylcypromine hydrochlorid (2 μM; 3 h) shows a specific derepression of OCT4 transcription[1].Tranylcypromine hydrochlorid (0-100 μM; 15 min) shows IC50values of 20.7, 2.3 and 0.95 μM for LSD1, MAO A and MAO B, respectively[2].Tranylcypromine hydrochlorid (0-800 μM) shows Kivalues of 242.7, 101.9 and 16 μM for LSD1, MAO A and MAO B, respectively[2].
Western Blot Analysis[1] Cell Line: | Sf21 insect cell line | Concentration: | 50 μM, 200 μM, 1 mM and 5 mM | Incubation Time: | 12-14 hours or 1 hour | Result: | Showed inhibitory activities of histone H3K4 demethylation and nucleosomal demethylation. |
RT-PCR[1] Cell Line: | P19 EC cell line | Concentration: | 2 μM | Incubation Time: | 3 hours | Result: | Decreased Oct4 mRNA levels. |
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体内研究 (In Vivo) | Tranylcypromine hydrochlorid (3 mg/kg; i.p. once daily for 3 days) decreases LPS-mediated microglial activation and proinflammatory cytokine COX-2 and IL-6 levels in wild-type mice[3].Tranylcypromine hydrochlorid (3 mg/kg; i.p. once daily for 7 days) down-regulates Aβ-mediate microglial activation in 5xFAD mice[3].
Animal Model: | Wild-type mice[3] | Dosage: | 3 mg/kg | Administration: | Intraperitoneal injection; 3 mg/kg once daily for 3 days | Result: | Significantly down-regulated LPS-stimulated microglial activation in the cortex and Hippocampus, and LPS-induced astrocyte activation only in the cortex. Reduced LPS-induced COX-2 levels in hippocampus CA1, decreased LPS-evoked IL-6 levels in the cortex and hippocampus CA1 and suppressed LPS-mediated IL-1β levels in the cortex. |
Animal Model: | 5xFAD mice[3] | Dosage: | 3 mg/kg | Administration: | Intraperitoneal injection; 3 mg/kg once daily for 7 days | Result: | Differentially regulated microglial and astrocyte activation in this mouse model of AD. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(589.45 mM;Need ultrasonic) DMSO : 100 mg/mL(589.45 mM;Need ultrasonic) 配制储备液 1 mM | 5.8945 mL | 29.4724 mL | 58.9449 mL | 5 mM | 1.1789 mL | 5.8945 mL | 11.7890 mL | 10 mM | 0.5894 mL | 2.9472 mL | 5.8945 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 (sealed storage, away from moisture)。-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: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (14.74 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.74 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-CDin saline) Solubility: ≥ 2.5 mg/mL (14.74 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.74 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (14.74 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.74 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。 *以上所有助溶剂都可在本网站选购。
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