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pristimerin

pristimerin Structure
CAS No.
1258-84-0
Chemical Name:
pristimerin
Synonyms
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
Molecular Formula:
C30H40O4
Molecular Weight:
464.64
MOL File:
1258-84-0.mol
Modify Date:
2023/9/15 15:02:29

pristimerin Properties

Melting point 219.5°C
Boiling point 488.1°C (rough estimate)
Density 1.0271 (rough estimate)
refractive index 1.4800 (estimate)
storage temp. -20°C
solubility DMSO: ≥5mg/mL
form Red solid
pka 8.60±0.70(Predicted)
color orange

SAFETY

Risk and Safety Statements

Toxicity LD50 oral in mouse: 8gm/kg

pristimerin price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) P0020 Pristimerin 1258-84-0 5MG ₹24183.05 2022-06-14 Buy
Sigma-Aldrich(India) P0020 Pristimerin 1258-84-0 25MG ₹96916.23 2022-06-14 Buy
Sigma-Aldrich(India) 530070 Pristimerin - CAS 1258-84-0 - Calbiochem A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii. 1258-84-0 5MG ₹9490 2022-06-14 Buy
Product number Packaging Price Buy
P0020 5MG ₹24183.05 Buy
P0020 25MG ₹96916.23 Buy
530070 5MG ₹9490 Buy

pristimerin Chemical Properties,Uses,Production

Description

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).

Uses

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

General Description

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).

Biological Activity

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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pristimerin Spectrum

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)- 1258-84-0 C30H40O4