Z-FY-CHO (Z-Phe-Tyr-CHO) 是一种有效且特异性的组织蛋白酶 L (CTSL) 抑制剂。
生物活性 | Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specificcathepsin L(CTSL)inhibitor[1][2]. |
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体外研究 (In Vitro) | Z-FY-CHO (10 μM, for 1 h) pretreatment alleviated cell death induced by 6-OHDA. Z-FY-CHO inhibits the increase in CTSL protein expression in 6-OHDA-treated SH-SY5Y cells. Treatment with Z-FY-CHO caused more LC3-II and less P62 expression in SH-SY5Y cells treated with 6-OHDA, indicating enhancing autophagy activity, and Z-FY-CHO blocks activation of caspase-3 and PARP[1]. Treatment with the specific cathepsin L inhibitor Z-FY-CHO (10 μM) or transfection with cathepsin L shRNA significantly increased the radiosensitivity of U251 cells. Both suppression and knockdown of cathepsin L in U251 cells increased irradiation-induced DNA damage and G2/M phase cell cycle arrest. Both suppression and knockdown of cathepsin L in U251 cells also increased irradiation-induced apoptosis, as shown by the increased levels of Bax and decreased levels of Bcl-2[2].
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体内研究 (In Vivo) | Intraperitoneal administration of Z-FY-CHO (2.5-10 mg/kg) for 4 weeks suppresses bone weight loss dose dependently in the ovariectomized mouse, experimental model of osteoporosis. Z-FY-CHO acts as a bone resorption suppressor through the inhibition of collagen degradation[3].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°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: DMSO : 100 mg/mL(223.96 mM;Need ultrasonic) 配制储备液 1 mM | 2.2396 mL | 11.1982 mL | 22.3964 mL | 5 mM | 0.4479 mL | 2.2396 mL | 4.4793 mL | 10 mM | 0.2240 mL | 1.1198 mL | 2.2396 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: ≥ 1.25 mg/mL (2.80 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.80 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 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: 1.25 mg/mL (2.80 mM); Suspended solution; Need ultrasonic
此方案可获得 1.25 mg/mL (2.80 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.80 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.80 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 12.5 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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