Z-LEHD-FMK TFA 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 TFA 在大鼠脊髓损伤模型中也表现出神经保护作用。
| 生物活性 | Z-LEHD-FMK TFA is a selective and irreversible inhibitor ofcaspase-9, protects against lethal reperfusion injury and attenuatesapoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma[1][2][3]. |
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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].
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. |
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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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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