pristimerin

Bezeichnung:pristimerin

CAS-Nr1258-84-0

Englisch Name:pristimerin

CBNumberCB41360260

SummenformelC30H40O4

Molgewicht464.64

MOL-Datei1258-84-0.mol

pristimerin physikalisch-chemischer Eigenschaften

Schmelzpunkt	219.5°C
Siedepunkt	488.1°C (rough estimate)
Dichte	1.0271 (rough estimate)
Brechungsindex	1.4800 (estimate)
storage temp.	-20°C
Löslichkeit	DMSO: ≥5mg/mL
Aggregatzustand	Red solid
pka	8.60±0.70(Predicted)
Farbe	orange

Sicherheit

Toxizität

LD50 oral in mouse: 8gm/kg

pristimerin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-arachidonoyl glycerol (2-AG), terminating its capacity to activate cannabinoid receptors. Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC₅₀ = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 μM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).
Verwenden
antineoplastic, antiinflammatory
Verwenden
Pristimerin is a triterpenoid that inhibits tumor angiogenesis by targeting VEGFR2 activation and is known to exhibit anti-inflammatory properties.
Definition
ChEBI: Pristimerin is a carboxylic ester.
Allgemeine Beschreibung
A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii, whose inhibitory activities against proteasome chymotrypsin subunit (IC₅₀ = 2.2 and 3.0 μM against purified rabbit 20S and human 26S proteasome, respectively) and cellular NF-κB pathway/IKK activation most likely account for its reported anticancer efficacy both in vitro (IC₅₀ ≤610 nM in A549, K562, KBM5, MCF-7, MDA-MB-231, HepG2, and primary human leukemia cell cultures) and in mice in vivo (1 to 2.5 mg/kg/day, s.c.), including imatinib/STI571-resistant cancer cells harboring Bcr-Abl T315I mutation. Also reported to inhibit the activity of monoacylglycerol lipase (MGL), the enzyme that hydrolyzes and deactivates the cannabionoid receptor ligand 2-Arachidonoyl-sn-glycerol (2-AG), in a reversible manner with high potency (IC₅₀ = 93 nM).
Biologische Aktivität
Potent and reversible inhibitor of monoacylglycerol lipase (MGL) (IC 50 = 93 nM). Also suppresses NF- κ B activation via inhibition of proteasome chymotrypsin-like activity and IKK α / β . Displays antitumor, anti-inflammatory and antimicrobial activities.

pristimerin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

1258-84-0, pristimerin Verwandte Suche:

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