BESTATIN HYDROCHLORIDE

Bezeichnung:BESTATIN HYDROCHLORIDE

CAS-Nr65391-42-6

Englisch Name:BESTATIN HYDROCHLORIDE

CBNumberCB2172341

SummenformelC16H25ClN2O4

Molgewicht344.83

MOL-Datei65391-42-6.mol

BESTATIN HYDROCHLORIDE physikalisch-chemischer Eigenschaften

Schmelzpunkt	216-218 °C
storage temp.	2-8°C
Löslichkeit	H₂O: 25 mg/mL, clear, colorless
Aggregatzustand	White to off-white powder.
Farbe	White
Wasserlöslichkeit	Soluble in water (4 mg/ml, warm), DMSO (>25 mg/ml), methanol, acetic acid, dimethyl formamide, and 100% ethanol.
BRN	4628066
Stabilität	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 Datenbank	65391-42-6(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	20/21/22-36/37/38
S-Sätze:	22-24/25-36-26
WGK Germany	3
F	3-10
HS Code	29242995

Gefahreninformationscode (GHS)

BESTATIN HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
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.
Verwenden
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.
Verwenden
competitive aminopeptidase B inhibitor
Verwenden
Bestatin Hydrochloride is an inhibitor of aminopeptidases, LAP3, and leukotriene A4 hydrolase. It is the salt form of Bestatin (B319500).
Verwenden
Bestatin has been used as a protease inhibitor for the purification of his-tagged Tau protein.
Definition
ChEBI: Bestatin (hydrochloride) is a peptide.
Allgemeine Beschreibung
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].
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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