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CAS No.: 1135695-98-5

Q-VD-OPh Catalog No. CSN17276

Synonyms: QVD-OPH;Quinoline-Val-Asp-Difluorophenoxymethylketone;Quinoline-Val-Asp-Difluorophenoxymethylketone. quinoline-val-asp(OMe)-CH2-OPH

Q-VD-OPh is a potent pan-caspase inhibitor of caspases 1, 3, 8, and 9 with IC50 values of 50, 25, 100, and 430 nM, respectively, showing inhibitory effects on terminal caspase activation, substrate cleavage, and DNA ladder formation associated with apoptosis.

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实验方案

技术信息

生物活性

描述Apoptosis is mediated by speciﬁc initiating and effector cysteine proteases (caspases) that are unique in cleaving substrates speciﬁcally following aspartate residues. The activation of speciﬁc caspases has deﬁned three major pathways that can carry out the apoptotic process^[6]. Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties, and it inhibits caspase 7 with IC₅₀ of 48 nM and 25 - 400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12^[7]. The broad spectrum caspase inhibitor, Boc-D-fmk, completely prevents apoptosis in WEHI 231 cells at 50 µM, but is ineffective at lower doses. In striking contrast, the caspase inhibitor Q-VD-OPh dramatically prevents DNA fragmentation at concentrations as low as 5 µM^[6]. Analysis of 5 µM Q-VD-OPh in the presence of actinomycin D in WEHI 231 cells for at least 48 h results in no change in the cell number and complete cellular viability as determined by cell number and trypan blue exclusion^[6]. Similar to WEHI 231 cells, the presence of 5 µM Q-VD-OPh completely prevents the actinomycin D-induced DNA fragmentation and apoptosis from occurring in Jurkat T cells^[6]. TGF beta induced apoptosis in HRP-1 cells within 24 h, as determined by DNA laddering, and this is completely inhibited by 5 µM Q-VD-OPh, consistent with other cell lines^[6]. C57BL/6 mice with ischemic ARF treated with Q-VD-OPh has a marked (100%) reduction in blood urea nitrogen (BUN) and serum creatinine and a highly significant reduction in morphological acute tubular necrosis (ATN) score compared with vehicle-treated mice^[8]. Two-day-old Swiss-Webster mice are infected with 10⁴ PFU of myocarditic virus, followed by the administration of Q-VD-Oph, Z-VAD(OMe)-FMK, or their diluent controls on days 3 to 6 postinfection. Mice receiving caspase inhibitors shows statistically signiﬁcant reductions in myocardial injury scores compared to controls, as measured by two independent myocardial injury scoring systems^[9].
动物研究
剂量
Mice: 20 mg/kg^[3] (i.p.) Rat: 0.4 mg/kg^[4] (i.p.), 1 mg/kg^[5] (i.p.); 0.1 mg/kg^[5] (neonatal stroke model, i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.p.) Rat: 0.4 mg/kg^[4] (i.p.), 1 mg/kg^[5] (i.p.); 0.1 mg/kg^[5] (neonatal stroke model, i.v.)
给药途径	i.p., i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9475 mL
- 9.7373 mL
- 19.4746 mL
- 5 mM
- 0.3895 mL
- 1.9475 mL
- 3.8949 mL
- 10 mM
- 0.1947 mL
- 0.9737 mL
- 1.9475 mL

技术信息

CAS号

1135695-98-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H25F2N3O6

运输

蓝冰

分子量

513.49

别名

QVD-OPH;Quinoline-Val-Asp-Difluorophenoxymethylketone;Quinoline-Val-Asp-Difluorophenoxymethylketone. quinoline-val-asp(OMe)-CH2-OPH

溶解度

DMSO	460.0 mg/mL (895.8 mM)
Water	insoluble

动物实验配方

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