|
| | BESTATIN HYDROCHLORIDE Basic information |
| Product Name: | BESTATIN HYDROCHLORIDE | | Synonyms: | N-[(2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTYRYL]-L-LEUCINE HYDROCHLORIDE;N-(3R-AMINO-2S-HYDROXY-1-OXO-4-PHENYLBUTYL)-L-LEUCINE, MONOHYDROCHLORIDE;[(2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTANOYL]-L-LEUCINE HCL;[(2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTANOYL]-L-LEUCINE HYDROCHLORIDE;(AMINO-2-HYDROXY-4-PHENYLBUTYRYL)-L-LEUCINE HYDROCHLORIDE;BESTATIN HCL;BESTATIN HYDROCHLORIDE;N-(2S,3R-3-AMINO-2-HYDROXY-4-PHENYLBUTY- RYL)-L-LEUCINE HCL | | CAS: | 65391-42-6 | | MF: | C16H25ClN2O4 | | MW: | 344.83 | | EINECS: | | | Product Categories: | peptides;Bestatin;Pepetides;inhibitor | | Mol File: | 65391-42-6.mol |  |
| | BESTATIN HYDROCHLORIDE Chemical Properties |
| Melting point | 216-218 °C | | storage temp. | 2-8°C | | solubility | H2O: 25 mg/mL, clear, colorless | | form | White to off-white powder. | | color | White | | Water Solubility | Soluble in water (4 mg/ml, warm), DMSO (>25 mg/ml), methanol, acetic acid, dimethyl formamide, and 100% ethanol. | | BRN | 4628066 | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO, distilled water, or ethanol may be stored at -20° for up to 1 month. | | InChIKey | XGDFITZJGKUSDK-UDYGKFQRSA-N | | CAS DataBase Reference | 65391-42-6(CAS DataBase Reference) |
| | BESTATIN HYDROCHLORIDE Usage And Synthesis |
| Description | Bestatin HCl (65391-42-6) inhibits leucine aminopeptidase and aminopeptidases B and N. Inhibits leukotriene A4 hydrolase. Displays immunostimulant activity via activation of macrophages and T lymphocytes. Displays antitumor activity. | | Uses | Bestatin Hydrochloride is an inhibitor of aminopeptidases, LAP3, and leukotriene A4 hydrolase. It is the salt form of Bestatin (B319500). | | Uses | competitive aminopeptidase B inhibitor | | Uses | Bestatin is an inhibitor of amino peptidases and a potent, irreversible inhibitor of LTA4 hydrolase. It inhibits the amino peptidase activity of LTA4 hydrolase with a Ki value of 201 nM. It offers promise as a novel analgesic because it protects endogenous opioid peptides against degradation. It does not inhibit carboxypeptidases. | | Uses | Bestatin has been used as a protease inhibitor for the purification of his-tagged Tau protein. | | Definition | ChEBI: Bestatin (hydrochloride) is a peptide. | | General Description | Chemical structure: amino acid derivatives | | Biochem/physiol Actions | A metalloprotease inhibitor selective for aminopeptidase. Bestatin is a competitive and specific inhibitor of leucine aminopeptidase, aminopeptidase B, and triamino peptidase. It inhibits aminopeptidase B at 60 nM (using arginine-β-naphthylamide as substrate) and leucine aminopeptidase at 20 nM (leucine-β-naphthylamide as substrate). It showed no inhibition of aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, or themolysin. It offers promise as a novel analgesic because it protects endogenous opioid peptides against degradation. | | in vivo | in a mouse dorsal air sac assay, oral administration of bestatin (100-200 mg/kg/day) showed a significant inhibitory activity against the melanoma cell-induced angiogenesis. bestatin also inhibited the tube-like formation of human umbilical vein endothelial cells (huvecs). furthermore, after the orthotopic implantation of b16-bl6 melanoma cells into mice, bestatin administration (50-100 mg/kg/day, i.p) reduced the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice [1]. | | References | 1) Orning et al. (1991), Leukotriene A4 hydrolase. Inhibition by bestatin and intrinsic aminopeptidase activity establish its functional resemblance to metallohydrolase enzymes; J. Biol. Chem., 266 1375
2) Wang et al. (2010), The effect of different species aminopeptidase N structure on the activity screening of aminopeptidase N inhibitor; Biol. Pharm. Bull., 33 1658 |
| | BESTATIN HYDROCHLORIDE Preparation Products And Raw materials |
|
