Z-LEHD-FMK

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Z-LEHD-FMK; 纯度: ge;98.0%

Z-LEHD-FMK 是一种选择性和不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减弱细胞凋亡。Z-LEHD-FMK 在大鼠脊髓损伤模型中也表现出神经保护作用。

Z-LEHD-FMKamp;;

Z-LEHD-FMK Chemical Structure

CAS No. : 210345-04-3

规格 价格 是否有货 数量
1 mg ￥9800 In-stock
5 mg ; 询价 ;
10 mg ; 询价 ;

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生物活性

Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma[1][2][3].

IC50 Target[1]

Caspase-9

;

体外研究
(In Vitro)

Z-LEHD-FMK (20 μM; pretreated for 30 min) completely protects HCT116 and 293 cells from TRAIL-induced toxicity[1].
Z-LEHD-FMK (20 μM ; 6 h) protects normal human hepatocytes from TRAIL-induced apoptosis[1].

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

Apoptosis Analysis[1]

Cell Line: SW480, H460, HCT116 and 293 cells
Concentration: 20 μM
Incubation Time: Pretreated for 30 min
Result: Protected HCT116 and 293 cells from TRAIL-induced apoptosis.

Western Blot Analysis[1]

Cell Line: HCT116, SW480 cells
Concentration: 20 μM
Incubation Time: 2 h
Result: Protected procaspase 3 from cleavage in HCT116 cells but not in SW480 cells, especially at the 16-h time point.

体内研究
(In Vivo)

Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) protects neurons, glia, myelin, axons, and intracellular organelles in spinal cord injury (SCI) rats[2].

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

Animal Model: Male Wistar albino rats (250-350 g) with SCI[2]
Dosage: 0.8 μmol/kg
Administration: I.v. for 1 or 7 days
Result: Decreased the mean apoptotic cell count at 24 hours and 7 days postinjury.

分子量

690.72

Formula

C32H43FN6O10
CAS 号

210345-04-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (144.78 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4478 mL 7.2388 mL 14.4776 mL
5 mM 0.2896 mL 1.4478 mL 2.8955 mL
10 mM 0.1448 mL 0.7239 mL 1.4478 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。
参考文献

  • [1]. Ozoren N, et, al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2000 Nov 15; 60(22): 6259-65.

    [2]. Colak A, et, al. Neuroprotection and functional recovery after application of the caspase-9 inhibitor z-LEHD-fmk in a rat model of traumatic spinal cord injury. J Neurosurg Spine. 2005 Mar; 2(3): 327-34.

    [3]. Mocanu MM, et, al. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May; 130(2): 197-200.