Pepstatin (Pepstatin A) 是由放线菌类产生的一种特异性的天冬氨酸蛋白酶 (aspartic proteases) 抑制剂，能够抑制 hemoglobin-pepsin，hemoglobin-proctase，casein-pepsin，casein-proctase，casein-acid protease 和 hemoglobin-acid protease 的活性，IC50 值分别为 4.5 nM，6.2 nM，150 nM，290 nM，520 nM 和 260 nM；同时可抑制 HIV protease 的活性。
| CAS No. | 26305-03-3 |
| 生物活性 | Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease. |
| 分子式 | C34H63N5O9 |
| 分子量 | 685.89 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -80°C 2 years |
| 溶解性数据 | DMSO : 125 mg/mL (182.24 mM; Need ultrasonic) |
| 体内研究 | Pepstatin (Pepstatin A) has a very low toxicity, with LD50s of 1090 mg/kg, 875 mg/kg, 820 mg/kg and 450 mg/kg for mice, rats, rabbits, and dogs by i.p. route, and > 2000 mg/kg for all species by oral route. Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats. |
| 体外研究 | Pepstatin (Pepstatin A) is a specific acid protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin (Pepstatin A) inhibits the recombinant HIV protease with an IC50 of 250 μM. Pepstatin shows no effect on cellular protein synthesis and probably does not exert severe cell toxicity. |
| 文献 | •Cell Rep. 2021 Nov 2;37(5):109931. •Environ Sci Technol. 2017 Dec 5;51(23):13938-13948. •Pharmacol Res. 2021 Dec 1;175:105985. •Int J Oncol. 2019 Jul;55(1):331-339. •Int J Antimicrob Agents. 2019 Dec;54(6):814-819. •FASEB J. 2022 Jan;36(1):e22121. •J Virol. 2021 Sep 22;JVI0153721. •Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. •Biochem Bioph Res Co. 2020 Sep 10;530(1):292-300. •Mol Med Rep. 2019 Jan;19(1):41-50. |
| 纯度及产品资料 | 98% |
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