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pristimerin

Product Name
pristimerin
CAS No.
1258-84-0
Chemical Name
pristimerin
Synonyms
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
Molecular Formula
C30H40O4
Formula Weight
464.64
MOL File
1258-84-0.mol
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pristimerin Property

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
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Safety

Toxicity
LD50 oral in mouse: 8gm/kg
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
P0020
Product name
Pristimerin
Purity
≥98% (HPLC)
Packaging
5mg
Price
$240
Updated
2024/03/01
Sigma-Aldrich
Product number
530070
Product name
Pristimerin
Packaging
5mg
Price
$172
Updated
2024/03/01
Cayman Chemical
Product number
13621
Product name
Pristimerin
Purity
≥98%
Packaging
5mg
Price
$97
Updated
2024/03/01
Cayman Chemical
Product number
13621
Product name
Pristimerin
Purity
≥98%
Packaging
10mg
Price
$184
Updated
2024/03/01
Sigma-Aldrich
Product number
PHL83303
Product name
Pristimerin
Purity
phyproof? Reference Substance
Packaging
10mg
Price
$514
Updated
2024/03/01
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pristimerin Chemical Properties,Usage,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

antineoplastic, antiinflammatory

Uses

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.

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 Suppliers

Canada 1 China 157 India 1 United Kingdom 1 United States 11 Global 171
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77
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View Lastest Price from pristimerin manufacturers

Hebei Yanxi Chemical Co., Ltd.
Product
Pristimerin 1258-84-0
Price
US $40.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
10 tons
Release date
2023-09-15
Shaanxi Dideu Medichem Co. Ltd
Product
Pristimerin 1258-84-0
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
99.0%
Supply Ability
10000KG
Release date
2024-08-09
Shanghai Standard Technology Co., Ltd.
Product
Pristimerin 1258-84-0
Price
US $0.00/mg
Min. Order
20mg
Purity
≥98%(HPLC)
Supply Ability
100 g
Release date
2020-08-18

1258-84-0, pristimerinRelated Search:

Cisplatin Carboplatin Arctiin 1-O-OCTADECYL-2-O-METHYL-SN-GLYCERO-3-PHOSPHOCHOLINE (-)-Arctigenin Oridonin Pyrrolcarbonyltaloside gamma-Linolenic acid Baccatine III Oxaliplatin Isorhamnetin FRIEDELAN-3BETA-OL lithospermic acid Taxifolin Celastrol alpha-Terpinene pristimerin 2,2,4,4,5,5,7,7-OCTAMETHYLOCTANE

  • 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