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Amastatin . hydrochloride Cat. No.: 10-016

Amastatin . hydrochloride

PREDICTED MOLECULAR WEIGHT:474.6 . 36.5

Properties

PURIFICATION: ?98% (HPLC)

PHYSICAL STATE: White to off-white powder.

Short Term Storage: +4°C. Long Term Storage: -20°C. Handling Advice: Keep cool and dry. STORAGE CONDITIONS: Protect from moisture. Use/Stability: Stable for at least 2 years after receipt when stored at -20°C.

Additional Info

ALTERNATE NAMES: [(2S,3R)-3-Amino-2-hydroxy-5-methyl-hexanoyl]-Val-Val-Asp-OH . HCl

Background and References

September 28, 2021 1 https://www.prosci-inc.com/amastatin-hydrochloride-10-016.html Slow, tight binding and competitive (AP) inhibitor. Inhibits cytosolic aminopeptidase, microsomal aminopeptidase M and bacterial leucine aminopeptidase, human serum aminopeptidase A (AP-A), aminopeptidase N (AP-N), tyrosine aminopeptidase, but not (AP-B). Amastatin is without effect on trypsin, papain, chymotrypsin, elastase, pepsin or thermolysin. Inhibits completely the Suc-Ala-Ala-Pro-Leu-pNA amidolytic enzyme. Slightly inhibits the formation of angiotensin III (Ang III) from Angiotensin II through AP-A, but significantly increases the potency of BACKGROUND: angiotensin III and [des-Asp1]-angiotensin I. Moderate inhibitor of mitochondrial intermediate peptidase (MIP). Weak inhibitor of simian immunodeficiency virus protease (SIV-PR). ANPEP (aminopeptidase N) is a host receptor targeted by porcine epidemic diarrhoea virus, human coronavirus 229E, feline coronavirus, canine coronavirus, transmissible gastroenteritis virus and infectious bronchitis virus. These viruses all belong to coronaviridae. ANPEP is therefore investigated as a potential target for SARS-CoV-2 infections.

1) Amastatin, an inhibitor of aminopeptidase A, produced by actinomycetes: T. Aoyagi, et REFERENCES: al.; J. Antibiot. 31, 636 (1978)

2) Inhibition of by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes: D.H. Rich, et al.; J. Med. Chem. 27, 417 (1984)

3) The slow, tight binding of bestatin and amastatin to aminopeptidases: S.H. Wilkes & J.M. Prescott; J. Biol. Chem. 260, 13154 (1985)

4) Inhibition of aminopeptidases by containing ketomethylene and hydroxyethylene amide bond replacements: S.L. Harbeson & D.H. Rich; J. Med. Chem. 32, 1378 (1989)

5) Role of aminopeptidase activity in the regulation of the pressor activity of circulating angiotensins: S. Ahmad & P.E. Ward; J. Pharmacol. Exp. Ther. 252, 643 (1990)

6) Purification and biochemical characterization of recombinant simian immunodeficiency virus protease and comparison to human immunodeficiency virus type 1 protease: S.K. Grant, et al.; Biochemistry 30, 8424 (1991)

7) Rat liver mitochondrial intermediate peptidase (MIP): purification and initial characterization: F. Kalousek, et al.; EMBO J. 11, 2803 (1992)

8) and amastatin induce V(1)-receptor-mediated suppression of excitatory transmission in the rat parabrachial nucleus: X. Chen & Q.J. Pittman; J. Neurophysiol. 82, 1689 (1999)

9) Inhibitors on an elastase-like enzyme activity catalyzing Suc-Ala-Ala-Pro-Leu-pNA amidolysis in human seminal plasma: Y. Matsuda, et al.; Arch. Androl. 44, 1 (2000)

10) The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure- based design, chemistry, and activity: J. Grembecka, et al.; J. Med. Chem. 46, 2641 (2003)

ANTIBODIES FOR RESEARCH USE ONLY.

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September 28, 2021 2 https://www.prosci-inc.com/amastatin-hydrochloride-10-016.html