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一般說明
Pepstatin water soluble is a semisynthetic product derived from microbial Pepstatin A by the addition of the tri-peptide Gly-Lys-Lys-OH. Pepstatin water soluble is a novel product that has the same protease inhibition activity as Pepstatin A, but with increased solubility in water and in physiological media. The increased water solubility provides new options for using this inhibitor in aqueous solutions. Pepstatin water soluble was first described by Austen at al,. The published Ki for inhibition of Pepsin activity is the same as Pepstatin A. While Pepstatin A is only sparingly soluble in water or PBS, the water soluble Pepstatin product is soluble in water and PBS at concentration of 60 mg/ml .
應用
Both Pepstatin A and Water soluble Pepstatin are potent inhibitors of aspartyl proteases. Both of them contain the unusual amino acid statine. Pepstatin A is an inhibitor of acid proteases (aspartyl peptidases). It forms a 1:1 complex with proteases such as pepsin, renin, , cathepsin D , bovine chymosin, and protease B (Aspergillus Niger).4 Solubilized γ-secretase6 and retroviral protease7 are also inhibited by Pepstatin A.
特點和優勢
- Same protease inhibition activity as Pepstatin A
- Icreased solubility in water and in physiological media
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
J Marciniszyn et al.
Advances in experimental medicine and biology, 95, 199-210 (1977-01-01)
Pepstatin is a low molecular weight, potent inhibitor specific for acid proteases with a Ki value of about 10(-10)M for pepsin. The chemical structure of pepstatin is essentially a hexapeptide which contains two residues of an unusual amino acid, 4-amino-3-hydroxy-6-methylheptanoic
Solid-phase synthesis of a soluble pepstatin derivative suitable for therapeutic use.
B M Austen et al.
Bioscience reports, 2(6), 427-432 (1982-06-01)
K Takahashi et al.
Journal of biochemistry, 80(3), 497-506 (1976-09-01)
Comparative studies have been made on the effects of diazoacetyl-DL-norleucine methyl ester (DAN), 1,2-epoxy-3-(p-nitrophenoxy)propane (EPNP) and pepstatin on acid proteases, including those from Acrocylindrium sp., Aspergillus niger, Aspergillus saitoi, Mucor pusillus, Paecilomyces varioti, Rhizopus chinensis, and Trametes sanguinea, and also
Structures and activities of protease inhibitors of microbial origin.
H Umezawa
Methods in enzymology, 45, 678-695 (1976-01-01)
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