Ucf-101
目录号 : KM3101 CAS No. : 313649-08-0 纯度 : 98%

Ucf-101 是一种选择性和竞争性的促凋亡蛋白酶 Omi/HtrA2 抑制剂,抑制 His-Omi 的 IC50 值为 9.5 μM。Ucf-101 对各种其他丝氨酸蛋白酶的活性极低 (IC50>200 μM)。Ucf-101 在 543 nm 处具有天然的红色荧光,可用于监视其进入哺乳动物细胞的能力。Ucf-101 对 MI/R 损伤具有明显的心脏保护作用,并且还具有一定的神经保护作用。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg 询价 In-stock
200mg 询价 In-stock

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生物活性

Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.

体外研究

Ucf-101 (20-100 μM; 30 min) inhibits the proteolytic activity of MBP-Omi-(134-458).
Ucf-101 (10-100 μM; pretreated for 10 min) inhibits His-Omi-(134-458) activity in a concentration-dependent manner when assayed with His-Omi-(134-458) and β-casein.
Ucf-101 (1-25 μM; 36 h) inhibits Omi-induced caspase-independent apoptosis of mouse embryo caspase-9 (-/-) null fibroblasts.
Ucf-101 (1-20 μM; pretreated for 1 h) inhibits the 6-OHDA-induced apoptosis of Parkinson’s disease (PD)-PC12 cells at the low concentration (2.5 μM), and increases the apoptosis rate at the high concentration (≥10 μM).
Ucf-101 (2.5 μM; pretreated for 1 h) downregulates the expression of Glucose-regulated protein 78 (Bip/Grp78) and C/EBP homologous protein (CHOP) in PD- PC12 cells.

体内研究

Ucf-101 (0.6-1.8 μmol/kg; a single i.p.) reduces postischemic myocardial apoptosis and myocardial infarct size in mice.
Ucf-101 (1.5 μmol/kg; a single i.p.) improves the APO-induced rotational behavior, increases the TH-positive cells and reverses the reduction of DA neurons in the PD rats.

Animal Model: Adult male mice (20-25 g) with myocardial ischemia/reperfusion (MI/R) injury
Dosage: 0.6, 1.5, 1.8 μmol/kg
Administration: I.p. 10 minutes before reperfusion
Result: Reduced terminal dUTP nick end-labeling staining, incidence of DNA ladder fragmentation, and infarct size.
分子式
C27H17N3O5S
分子量
495.51
CAS号
313649-08-0
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: 

DMSO : 12.5 mg/mL (25.23 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0181 mL 10.0906 mL 20.1812 mL
5 mM 0.4036 mL 2.0181 mL 4.0362 mL
10 mM 0.2018 mL 1.0091 mL 2.0181 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    90% (20% SBE-β-CD in saline)

    Solubility: 1.79 mg/mL (3.61 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.79 mg/mL (3.61 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 17.9 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.67 mg/mL (3.37 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.67 mg/mL (3.37 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 16.7 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。

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