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  2. Bacterial
  3. Pristimerin

Pristimerin (Synonyms: Celastrol methyl ester)

Cat. No.: HY-N1937 Purity: 99.64%
Handling Instructions

Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.

For research use only. We do not sell to patients.

Pristimerin Chemical Structure

Pristimerin Chemical Structure

CAS No. : 1258-84-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 324 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.

IC50 & Target

IC50: 93 nM (MGL)[1]

In Vitro

Pristimerin inhibits the activity of purified MGL with an IC50 of 93±8 nM and that of non-purified MGL (cell lysates of MGL-transfected HeLa cells) with an IC50 of 398±68 nM. Pristimerin inhibits MGL through a mechanism that is rapid, reversible and non-competitive. The binding of pristimerin to MGL might be strengthened by formation of a polar interaction with a regulatory cysteine, possibly Cys208[1]. Pristimerin inhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner. Pristimerin decreases VEGF-induced autophosphorylation of VEGFR2 and attenuates the activation of the VEGF-induced VEGFR2-mediated signaling pathway [2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pristimerin inhibits inflammation and tumor angiogenesis. Pristimerin significantly reduces vessel density in synovial membrane tissues of inflamed joints and reduces the expression of pro-angiogenic factors in sera, including TNF-α, Ang-1, and MMP-9[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

464.64

Formula

C₃₀H₄₀O₄

CAS No.
SMILES

C[[email protected]](C1=CC=C(C(C)=C2O)C3=CC2=O)(CC[[email protected]]4(C)[[email protected]@]5([H])C[[email protected]@](C(OC)=O)(C)CC4)[[email protected]]5(CC[[email protected]]13C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (43.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1522 mL 10.7610 mL 21.5220 mL
5 mM 0.4304 mL 2.1522 mL 4.3044 mL
10 mM 0.2152 mL 1.0761 mL 2.1522 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (4.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

HFLS-RA (5 × 103 cells/mL) or HUVECs (1 × 104 cells/well) are seeded in 96-well plates and cultured in normal growth medium for 24 h. The cells are then incubated with different Pristimerin concentrations (0, 0.125, 0.25, 0.5 μM). The effects of Pristimerin on HUVECs viability are determined under VEGF-induced conditions. Cell viability is quantified by MTT assay. At 4 h before the end of the culture period, 30 μL of MTT solution (5.0 mg/mL) is added to each well. Cells without Pristimerin or VEGF served as a vehicle control[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Rat: Pristimerin is dissolved in DMSO (0.4%) and intraperitoneally injected daily into Male Sprague-Dawley rats in the experimental group (low-dose group, 0.40 mg/kg of body weight; high-dose group, 0.80 mg/kg of body weight) from day 11 to day 24 of immunization. The model group received vehicle (DMSO, 0.4%), and the normal control group received normal saline (NS). Methotrexate (positive control) is suspended in NS and orally administered in the autoimmune phase at an interval of 5 days[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

PristimerinCelastrol methyl esterBacterialInhibitorinhibitorinhibit

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Pristimerin
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