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| 中文名 | 乙酰基-天冬氨酰-谷氨酰-缬氨酰-天冬氨醛 |
|---|---|
| 英文名 | ac-devd-cho |
| 英文别名 | N-Acetyl-Asp-Glu-Val-Asp-al |
| 描述 | Ac-DEVD-CHO 是一种特异性 Caspase-3 抑制剂,Ki 值为 230 pM. |
|---|---|
| 相关类别 | |
| 靶点 |
Caspase 3:0.23 nM (Ki) Caspase-8:0.92 nM (Ki) Caspase-7:1.6 nM (Ki) Caspase-10:12 nM (Ki) Caspase-1:18 nM (Ki) Caspase-6:31 nM (Ki) Caspase-9:60 nM (Ki) Caspase-4:132 nM (Ki) Caspase-5:205 nM (Ki) Caspase-2:1710 nM (Ki) |
| 体外研究 | 为了确定胱天蛋白酶-3在SLNT诱导的细胞凋亡中的作用,使用半胱天冬酶-3抑制剂(Ac-DEVD-CHO)。添加Ac-DEVD-CHO可显着预防SLNT诱导的细胞凋亡(从32.91±1.21％降至15.88±1.58％,而NC和Ac-DEVD-CHO组分别为6.45±0.96％,7.77±0.79％)[2] ]。经金丝桃素介导的PDT处理后,经zVAD-fmk(5.32％)或Ac-DEVD-CHO(7.43％)预处理的细胞凋亡率明显下降[3]。值得注意的是,10μmol/ L Ac-DEVD-CHO部分阻断了SIN诱导的细胞凋亡的作用并减少了凋亡细胞核的数量。 SIN的这些作用被胱天蛋白酶-3抑制剂Ac-DEVD-CHO阻断。喜树碱(4μM)是一种阳性对照,可增加caspase-3活性,这也被Ac-DEVD-CHO阻断[4]。 |
| 体内研究 | 与模型组比较,CI组血清BUN浓度在术后各时间点均明显降低,6小时后Cr明显降低,12小时和24小时恢复为假手术组;在所有时间点,血清TNF-α,IL-6浓度均降低,IL-10浓度显着升高。 [TNF-α(μg/ L)6小时：436.2±64.2对比653.6±8.9,12小时：233.4±85.4对比579.7±137.1,24小时：151.0±90.3对比551.0±119.8,IL-6(μg)/L)6小时：1033.2±345.8对比1 595.3±159.4,12小时：366.3±68.3对比1 330.7±249.8,24小时：241.2±208.4对比815.3±572.7,IL-10(μg/ L)6小时：33.6±10.4对比26.6±4.5,12小时：37.2±5.0对比24.5±4.3,24小时：38.3±5.5对比18.2±1.6,所有P <0.05];肾细胞凋亡率在所有时间点均显着下降：凋亡率为6小时：(13.9±3.2)％对比(18.3±1.4)％,12小时：(10.5±3.6)％对比(15.9±3.5)％ ,24小时：(8.4±1.8)％vs.(12.5±2.1)％[5]。 |
| 细胞实验 | 将OCL与RANKL一起温育，并用含有或不含特异性半胱天冬酶-3抑制剂Ac-DEVD-CHO（10μM）的0.5mM SIN处理24小时。在处理结束时，用PBS洗涤细胞，并用10μMHoechst33258染料染色15分钟。用荧光显微镜捕获staineing细胞的图像。通过计数每个孔中具有凋亡核浓缩的细胞数来评估差异[4]。 |
| 动物实验 | 对102只雄性小鼠进行盲肠结扎和穿刺或假手术。根据随机数表将动物分成三个相等的组（n = 34）：假手术组，模型组和半胱天冬酶-3抑制剂（CI）组。在CLP前30分钟，在CI组中皮下注射Ac-DEVD-CHO（4μg/ g）。测定血尿素氮（BUN）和肌酐（Cr）水平，用酶联免疫吸附试验测定肿瘤坏死因子-α（TNF-α），白细胞介素（IL-6和IL-10）的浓度（ ELISA），通过流式细胞术测定肾细胞凋亡率。观察三组小鼠的4天和7天存活率[5]。 |
| 参考文献 |
| 密度 | 1.374g/cm3 |
|---|---|
| 沸点 | 1021.1ºC at 760mmHg |
| 分子式 | C20H30N4O11 |
| 分子量 | 502.47200 |
| 闪点 | 571.3ºC |
| 精确质量 | 502.19100 |
| PSA | 245.37000 |
| 蒸汽压 | 0mmHg at 25°C |
| 折射率 | 1.535 |
| 储存条件 | -20°C |
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SECTION 1: Identification of the substance/mixture and of the company/undertaking Product identifiers Product name: N-Acetyl-Asp-Glu-Val-Asp-al REACH No.: A registration number is not available for this substance as the substance or its uses are exempted from registration, the annual tonnage does not require a registration or the registration is envisaged for a later registration deadline.
CAS-No.: 169332-60-9 Relevant identified uses of the substance or mixture and uses advised against Identified uses: Laboratory chemicals, Manufacture of substances SECTION 2: Hazards identification Classification of the substance or mixture Not a hazardous substance or mixture according to Regulation (EC) No. 1272/2008. This substance is not classified as dangerous according to Directive 67/548/EEC. Label elements The product does not need to be labelled in accordance with EC directives or respective national laws. Other hazards - none SECTION 3: Composition/information on ingredients Substances Synonyms: Ac-DEVD-CHO Formula: C20H30N4O11 Molecular Weight: 502,47 g/mol CAS-No.: 169332-60-9 No components need to be disclosed according to the applicable regulations. SECTION 4: First aid measures Description of first aid measures If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. In case of skin contact Wash off with soap and plenty of water. In case of eye contact Flush eyes with water as a precaution. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Most important symptoms and effects, both acute and delayed The most important known symptoms and effects are described in the labelling (see section 2.2) and/or in section 11 Indication of any immediate medical attention and special treatment needed no data available SECTION 5: Firefighting measures Extinguishing media Suitable extinguishing media Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Special hazards arising from the substance or mixture Carbon oxides, nitrogen oxides (NOx) Advice for firefighters Wear self contained breathing apparatus for fire fighting if necessary. Further information no data available SECTION 6: Accidental release measures Personal precautions, protective equipment and emergency procedures Avoid dust formation. Avoid breathing vapours, mist or gas. For personal protection see section 8. Environmental precautions Do not let product enter drains. Methods and materials for containment and cleaning up Sweep up and shovel. Keep in suitable, closed containers for disposal. Reference to other sections For disposal see section 13. SECTION 7: Handling and storage Precautions for safe handling Provide appropriate exhaust ventilation at places where dust is formed. For precautions see section 2.2. Conditions for safe storage, including any incompatibilities Store in cool place. Keep container tightly closed in a dry and well-ventilated place. Recommended storage temperature: -20 °C Specific end use(s) Apart from the uses mentioned in section 1.2 no other specific uses are stipulated SECTION 8: Exposure controls/personal protection Control parameters Components with workplace control parameters Exposure controls Appropriate engineering controls General industrial hygiene practice. Personal protective equipment Eye/face protection Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin protection The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. Body Protection Choose body protection in relation to its type, to the concentration and amount of dangerous substances, and to the specific work-place., The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Respiratory protection Respiratory protection is not required. Where protection from nuisance levels of dusts are desired, use type N95 (US) or type P1 (EN 143) dust masks. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). Control of environmental exposure Do not let product enter drains. SECTION 9: Physical and chemical properties Information on basic physical and chemical properties a) AppearanceForm: powder b) Odourno data available c) Odour Thresholdno data available d) pHno data available e) Melting point/freezingno data available point f) Initial boiling point and no data available boiling range g) Flash pointno data available h) Evapouration rateno data available i) Flammability (solid, gas) no data available j) Upper/lowerno data available flammability or explosive limits k) Vapour pressureno data available l) Vapour densityno data available m) Relative densityno data available n) Water solubilityno data available o) Partition coefficient: n- no data available octanol/water p) Auto-ignitionno data available temperature q) Decompositionno data available temperature r) Viscosityno data available s) Explosive propertiesno data available t) Oxidizing propertiesno data available Other safety information no data available SECTION 10: Stability and reactivity Reactivity no data available Chemical stability Stable under recommended storage conditions. Possibility of hazardous reactions no data available Conditions to avoid no data available Incompatible materials Strong acids, Strong bases Hazardous decomposition products Other decomposition products - no data available In the event of fire: see section 5 SECTION 11: Toxicological information Information on toxicological effects Acute toxicity no data available Skin corrosion/irritation no data available Serious eye damage/eye irritation no data available Respiratory or skin sensitisation no data available Germ cell mutagenicity no data available Carcinogenicity IARC:No component of this product present at levels greater than or equal to 0.1% is identified as probable, possible or confirmed human carcinogen by IARC. Reproductive toxicity no data available Specific target organ toxicity - single exposure no data available Specific target organ toxicity - repeated exposure no data available Aspiration hazard no data available Additional Information RTECS: Not available To the best of our knowledge, the chemical, physical, and toxicological properties have not been thoroughly investigated. SECTION 12: Ecological information Toxicity no data available Persistence and degradability no data available Bioaccumulative potential no data available Mobility in soil no data available Results of PBT and vPvB assessment PBT/vPvB assessment not available as chemical safety assessment not required/not conducted Other adverse effects no data available SECTION 13: Disposal considerations Waste treatment methods Product Offer surplus and non-recyclable solutions to a licensed disposal company. Contaminated packaging Dispose of as unused product. SECTION 14: Transport information UN number ADR/RID: -IMDG: -IATA: - UN proper shipping name ADR/RID: Not dangerous goods IMDG: Not dangerous goods IATA:Not dangerous goods Transport hazard class(es) ADR/RID: -IMDG: -IATA: - Packaging group ADR/RID: -IMDG: -IATA: - Environmental hazards ADR/RID: noIMDG Marine pollutant: noIATA: no Special precautions for user no data available SECTION 15 - REGULATORY INFORMATION N/A SECTION 16 - ADDITIONAL INFORMATION N/A |
| 个人防护装备 | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| 危险品运输编码 | NONH for all modes of transport |
| WGK德国 | 3 |