Pepstatin (Pepstatin A) 是由放线菌类

Pepstatin (Pepstatin A) is a specific, orally active 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 also inhibits HIV protease^[1][2].

IC50: 4.5 nM (Hemoglobin-pepsin), 6.2 nM (Hemoglobin-proctase), 150 nM (Casein-pepsin), 260 nM (Hemoglobin-acid protease), 290 nM (Casein-proctase), 520 nM (Casein-acid protease)^[1]

Pepstatin (Pepstatin A) (7 μM; 48 h) affects the intracellular processing of HIV-specific gag protein^[2].

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^[1].
Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

685.89

C₃₄H₆₃N₅O₉

26305-03-3

IsoValeryl-Val-Val-Sta-Ala-Sta-OH

IsoVeryl-VV-Sta-A-Sta-OH

胃酶抑素；抑肽素；胃蛋白酶抑制剂；胃酶抑素A

• Others

actinomycetes

Room temperature in continental US; may vary elsewhere.

DMSO : 41.67 mg/mL (60.75 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

  Solubility: 2.08 mg/mL (3.03 mM); Clear solution; Need ultrasonic

• 2.

  请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (3.03 mM); Clear solution

• 3.

  请依序添加每种溶剂： 10% DMSO 90% corn oil

  Solubility: ≥ 2.08 mg/mL (3.03 mM); Clear solution

• [1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62. Content Brief

  [2]. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6. Content Brief