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My CartCAS：187389-52-2
Storage：Powder:-20℃，1 year;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 187389-52-2 |
| Name | Z-VAD(OMe)-FMK |
| Molecular Formula | C22H30FN3O7 |
| Molecular Weight | 467.49 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，1 year;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00010870 |
| SMILES | O=C(CF)[C@H](CC(OC)=O)NC([C@H](C)NC([C@H](C(C)C)NC(OCC1=CC=CC=C1)=O)=O)=O |
| InChIKey | MIFGOLAMNLSLGH-QOKNQOGYSA-N |
| InChI | InChI=1S/C22H30FN3O7/c1-13(2)19(26-22(31)33-12-15-8-6-5-7-9-15)21(30)24-14(3)20(29)25-16(17(27)11-23)10-18(28)32-4/h5-9,13-14,16,19H,10-12H2,1-4H3,(H,24,30)(H,25,29)(H,26,31)/t14-,16-,19-/m0/s1 |
| PubChem CID | 5497174 |
| Target Point | Caspase |
| Passage | Apoptosis |
| Background | Z-VAD-FMK is an irreversible pan-caspase inhibitor. Is a ubiquitin C-terminal hydrolase L1 (UCHL1) inhibitor. |
| Biological Activity | Z-VAD(OMe)-FMK 是一种可渗透细胞的不可逆 pan-caspase 抑制剂。Z-VAD（OMe）-FMK是一种广谱半胱天冬酶抑制剂，已被证明可抑制半胱天冬酶样蛋白酶的细胞内活化。[1-3] |
| In Vitro | 注射Z-VAD(OMe)-FMK可抑制肺组织中caspase-3的活性，并显著降低末端dUTP缺口末端标记阳性细胞的数量[1]。在SAH之前1小时和之后6小时腹膜内施用Z-VAD(OMe)-FMK。检查胱天蛋白酶-3和阳性TUNEL的表达作为细胞凋亡的标志物。 Z-VAD(OMe)-FMK抑制内皮细胞中的TUNEL和caspase-3染色，降低caspase-3活化，降低BBB通透性，缓解血管痉挛，消除脑水肿，并改善神经功能[2]。 Z-VAD(OMe)-FMK是一种细胞渗透性半胱天冬酶抑制剂，可有效阻断SMN缺乏引起的细胞死亡[3]。 |
| In Vivo | 注射Z-VAD(OMe)-FMK可显著延长小鼠的存活率。所有小鼠在30小时内死于LPS。相比之下，用Z-VAD(OMe)-FMK治疗的小鼠存活时间显著更长，27％的小鼠存活超过7天[1]。 |
| Animal Experiment | 小鼠[1]本研究中使用的小鼠是5至6周龄(20至22克)ICR男性。通过尾静脉从大肠杆菌血清型O111：B4向小鼠注射30mg/kg LPS。在LPS注射前15分钟进行单次静脉内注射Z-VAD(OMe)-FMK(0.25mg)，然后每小时静脉内注射三次Z-VAD(OMe)-FMK(每次0.1mg)。对照小鼠用无菌盐水中相同体积的1％DMSO注射。大鼠[2]用α-氯醛糖(40mg/kg IP)和尿烷(400mg/kg IP)麻醉重300-350g的雄性Sprague-Dawley大鼠。对动物进行插管，并用小型动物呼吸器维持呼吸。使用加热垫将直肠温度维持在37±0.5°C。分离左外颈动脉，并通过颈内动脉插入4.0单丝尼龙缝合线以穿透大脑中动脉。在每只大鼠尸检时确认SAH。假手术的大鼠经历相同的程序，除了在感觉到抵抗后撤回缝合线。在SAH诱导前1小时和6小时腹膜内注射Z-VAD(OMe)-FMK(每0.3mL50μM)。在赋形剂组中，对大鼠进行SAH诱导，并用相同体积的载体(在生理缓冲液中稀释的DMSO)处理。在假手术动物中不进行任何治疗。 |
| Data Literature Source | [1]. Kawasaki M，et al. Protection from lethal apoptosis in lipopolysaccharide-induced acute lung injury in mice by a caspaseinhibitor. Am J Pathol. 2000 Aug;157(2):597-603. [2]. Park S，et al. Neurovascular protection reduces early brain injury after subarachnoid hemorrhage. Stroke. 2004 Oct;35(10):2412-7. [3]. Ilangovan R，et al. Inhibition of apoptosis by Z-VAD-fmk in SMN-depleted S2 cells. J Biol Chem. 2003 Aug 15;278(33):30993-9. |
| Unit | Bottle |
| Specification | 1mg 5mg |
是一种不可逆的 pan-caspase 抑制剂。是泛素 C 末端水解酶 L1 (UCHL1) 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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Alfhili MA, et. . Int J Occup Med Environ Health. 2022 Feb 15;35(1):1-11. doi: 10.13075/ijomeh.1896.01814.
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