프리스티메린

프리스티메린
프리스티메린 구조식 이미지
카스 번호:
1258-84-0
한글명:
프리스티메린
동의어(한글):
프리스티메린
상품명:
pristimerin
동의어(영문):
pristimerin;Pristimerine;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;(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
CBNumber:
CB41360260
분자식:
C30H40O4
포뮬러 무게:
464.64
MOL 파일:
1258-84-0.mol
MSDS 파일:
SDS

프리스티메린 속성

녹는점
219.5°C
끓는 점
488.1°C (rough estimate)
밀도
1.0271 (rough estimate)
굴절률
1.4800 (estimate)
저장 조건
-20°C
용해도
DMSO: ≥5mg/mL
물리적 상태
빨간색 고체
산도 계수 (pKa)
8.60±0.70(Predicted)
색상
오렌지 레드
색상
오렌지색

안전

독성 LD50 oral in mouse: 8gm/kg

프리스티메린 C화학적 특성, 용도, 생산

개요

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).

용도

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

일반 설명

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).

생물학적 활성

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.

프리스티메린 준비 용품 및 원자재

원자재

준비 용품


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