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pristimerin

pristimerin Struktur
1258-84-0
CAS-Nr.
1258-84-0
Englisch Name:
pristimerin
Synonyma:
pristimerin;Pristimerine;Pristimerin-RM;Celastrol-methylether;Pristimerin(NSC 99281);Celastrol methyl ester;Pristimerin - CAS 1258-84-0 - Calbiochem;3-Hydroxy-2-oxo-24-nor-D:A-friedoolean-1(10),3,5,7-tetren-29-oic acid methyl ester;3-hydroxy-9β,13α-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid, methyl ester;(9β,13α,14β,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oicacidmethylester
CBNumber:
CB41360260
Summenformel:
C30H40O4
Molgewicht:
464.64
MOL-Datei:
1258-84-0.mol

pristimerin Eigenschaften

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

Sicherheit

Toxizit?t 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

Pristimerin is a triterpenoid that inhibits tumor angiogenesis by targeting VEGFR2 activation and is known to exhibit anti-inflammatory properties.

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 Aktivit?t

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


pristimerin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 171)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Shaanxi Dideu Medichem Co. Ltd
+86-29-81148696 +86-15536356810
1022@dideu.com China 3882 58
Hebei Yanxi Chemical Co., Ltd.
+8617531190177
peter@yan-xi.com China 5858 58
Shanghai Zheyan Biotech Co., Ltd.
18017610038
zheyansh@163.com CHINA 3619 58
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29886 58
Chengdu GLP biotechnology Co Ltd
028-87075086 13350802083
scglp@glp-china.com CHINA 1824 58
Chengdu Biopurify Phytochemicals Ltd.
+8618080483897
sales@biopurify.com China 3772 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28172 58
Shaanxi Pioneer Biotech Co., Ltd .
+8613259417953
sales@pioneerbiotech.com China 3000 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58
Shanghai Standard Technology Co., Ltd.
18502101150
ft-sales@nature-standard.com CHINA 1923 58

1258-84-0()Verwandte Suche:


  • pristimerin
  • 3-Hydroxy-2-oxo-24-nor-D:A-friedoolean-1(10),3,5,7-tetren-29-oic acid methyl ester
  • Celastrol-methylether
  • (9β,13α,14β,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oicacidmethylester
  • (9b,13a,14b,20a)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tertraen-29-oic acid methyl ester
  • 3-hydroxy-9β,13α-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid, methyl ester
  • Celastrol methyl ester
  • Pristimerin(NSC 99281)
  • Pristimerine
  • Pristimerin - CAS 1258-84-0 - Calbiochem
  • 24,25,26-Trinoroleana-1(10),3,5,7-tetraen-29-oic acid, 3-hydroxy-9,13-dimethyl-2-oxo-, methyl ester, (9β,13α,14β,20α)-
  • Methyl (2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylate
  • Pristimerin-RM
  • 1258-84-0
  • C30H40O4
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