Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) 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。
| 生物活性 |
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) 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.
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IC50 Target |
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]
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体外研究
(In Vitro) |
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) 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[1]. 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[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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体内研究
(In Vivo) |
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) 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[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 |
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| Formula |
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| Sequence |
IsoValeryl-Val-Val-Sta-Ala-Sta-OH
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| Sequence Shortening |
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| 中文名称 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Sealed storage, away from moisture
| Powder |
-80deg;C |
2 years |
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-20deg;C |
1 year |
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
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| 溶解性数据 |
In Vitro:;
DMSO : 32 mg/mL (40.00 mM; Need warming)
H2O : < 0.1 mg/mL (insoluble)
配制储备液
| 浓度 溶剂体积 质量 |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.2501 mL |
6.2506 mL |
12.5013 mL |
| 5 mM |
0.2500 mL |
1.2501 mL |
2.5003 mL |
| 10 mM |
0.1250 mL |
0.6251 mL |
1.2501 mL |
*
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 (sealed storage, away from moisture)。-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。
In Vivo:
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
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1.
请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline
Solubility: ≥ 2.08 mg/mL (2.60 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
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2.
请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (2.60 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (2.60 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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3.
请依序添加每种溶剂：;10% DMSO ;; 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.60 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.60 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在 MCE 网站选购。
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| 参考文献 |
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[1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.
[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.
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