Pristimerin (Synonyms: Celastrol methyl ester)

Name: Pristimerin
Brand: MedChemExpress
SKU: HY-N1937
Rating: 5.0 (7 reviews)

Cat. No.: HY-N1937 Purity: 99.81%: Data Sheet
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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.

CAS No. : 1258-84-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 7 publication(s) in Google Scholar

Other Forms of Pristimerin:

Celastrol In-stock
Pristimerin (Standard) Get quote

7 Publications Citing Use of MCE Pristimerin

•Mol Med Rep. 2025 Jun;31(6):153. [Abstract]

Cell Proliferation/Viability Assay

Cell Imaging/Staining

Histological Imaging/Staining

RT-PCR

: Pristimerin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Dec 8. [Abstract]; Representative blots and c densitometric quantification of p65 and p-p65 in cultured cells transfected with siPFKFB3 in the presence of NF-κB inhibitors, Pristimerin (500 nM) and IT901 (150 nM).

: Pristimerin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Dec 8. [Abstract]; Senescence-associated β-galactosidase (SA-β-Gal) staining in the presence of Pristimerin (500 nM) and IT901.

: Pristimerin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Dec 8. [Abstract]; mRNA expression of pro-inflammatory factors in cultured chondrocytes transfected with siPFKFB3 in the presence of Pristimerin (500 nM).

: Pristimerin purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2024 Nov 27:18:5445-5459. [Abstract]; Cells were treated by several concentrations Pristimerin (pri) (25 nM, 50 nM, 100 nM, 200 nM, 400 nM, 800 nM, 1000 nM, 2000 nM, 4000 nM) for 24 or 48 h. The viability of chondrocytes was assessed by CCK-8 assay.

: Pristimerin purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2024 Nov 27:18:5445-5459. [Abstract]; Hematoxylin-Eosin staining of cartilage Pristimerin (Pri) (200 nM) treatment.

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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]

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	ED₅₀	0.11 μg/mL Compound: 7	Cytotoxicity against human 1A9 cells after 6 days by SRB assay Cytotoxicity against human 1A9 cells after 6 days by SRB assay	[PMID: 14640511]
1A9	ED₅₀	0.1 μg/mL Compound: 7	Cytotoxicity against human 1A9 cells after 3 days by SRB assay Cytotoxicity against human 1A9 cells after 3 days by SRB assay	[PMID: 14640511]
1A9/ptx-10	ED₅₀	0.076 μg/mL Compound: 7	Cytotoxicity against human 1A9/PTX10 cells after 6 days by SRB assay Cytotoxicity against human 1A9/PTX10 cells after 6 days by SRB assay	[PMID: 14640511]
1A9/ptx-10	ED₅₀	0.11 μg/mL Compound: 7	Cytotoxicity against human 1A9/PTX10 cells after 3 days by SRB assay Cytotoxicity against human 1A9/PTX10 cells after 3 days by SRB assay	[PMID: 14640511]
A549	ED₅₀	0.31 μg/mL Compound: 7	Cytotoxicity against human A549 cells after 3 days by SRB assay Cytotoxicity against human A549 cells after 3 days by SRB assay	[PMID: 14640511]
A549	IC₅₀	1.03 μM Compound: 1	Cytotoxic activity against human A549 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human A549 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
A549	IC₅₀	1.1 μM Compound: 1a	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
A549	IC₅₀	1.4 μM Compound: CEL01	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
A549	IC₅₀	2.6 μM Compound: 1	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 39106494]
Bel-7402	IC₅₀	1.16 μM Compound: 1	Cytotoxic activity against human Bel7402 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human Bel7402 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
Bel-7402	IC₅₀	2.2 μM Compound: 1	Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 39106494]
HCT-8	ED₅₀	0.15 μg/mL Compound: 7	Cytotoxicity against human HCT8 cells after 3 days by SRB assay Cytotoxicity against human HCT8 cells after 3 days by SRB assay	[PMID: 14640511]
HL-60	IC₅₀	0.2 μM Compound: 23	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 21090801]
HT-29	IC₅₀	4600 ng/mL Compound: 6	Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay	[PMID: 9644053]
HeLa	IC₅₀	0.32 μM Compound: 1	Cytotoxic activity against human HeLa cells incubated for 48 hrs by MTT assay Cytotoxic activity against human HeLa cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
HeLa	IC₅₀	3.42 μM Compound: B, triterpene quinine methide	Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23395966]
HepG2	IC₅₀	0.78 μM Compound: 1	Cytotoxic activity against human HepG2 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human HepG2 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
Huh-7	CC₅₀	> 6.25 μM Compound: GNF-Pf-476	NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)	[PMID: 18579783]
KB	ED₅₀	0.1 μg/mL Compound: 7	Cytotoxicity against human KB cells after 3 days by SRB assay Cytotoxicity against human KB cells after 3 days by SRB assay	[PMID: 14640511]
KB	IC₅₀	0.55 μg/mL Compound: 5	Cytotoxicity against human KB cells by MTT assay Cytotoxicity against human KB cells by MTT assay	[PMID: 7714534]
KB	IC₅₀	0.9 μM Compound: 1a	Antiproliferative activity against human KB cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human KB cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
L1210	IC₅₀	0.36 μg/mL Compound: 5	Cytotoxicity against mouse L1210 cells by MTT assay Cytotoxicity against mouse L1210 cells by MTT assay	[PMID: 7714534]
MCF-10A	IC₅₀	0.8 μM Compound: 1	Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 39106494]
MCF7	ED₅₀	0.14 μg/mL Compound: 7	Cytotoxicity against human MCF7 cells after 3 days by SRB assay Cytotoxicity against human MCF7 cells after 3 days by SRB assay	[PMID: 14640511]
MCF7	IC₅₀	0.4 μM Compound: 23	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 21090801]
MCF7	IC₅₀	0.87 μM Compound: B, triterpene quinine methide	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23395966]
MCF7	IC₅₀	0.9 μM Compound: 1a	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
MCF7	IC₅₀	1.57 μM Compound: CEL01	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
MCF7	IC₅₀	3 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 39106494]
MDA-MB-231	IC₅₀	0.8 μM Compound: 1a	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
P388	IC₅₀	0.12 μg/mL Compound: 5	Cytotoxicity against mouse P388 cells by MTT assay Cytotoxicity against mouse P388 cells by MTT assay	[PMID: 7714534]
PANC-1	IC₅₀	1.49 μM Compound: CEL01	Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
PC-3	ED₅₀	0.23 μg/mL Compound: 7	Cytotoxicity against human PC3 cells after 3 days by SRB assay Cytotoxicity against human PC3 cells after 3 days by SRB assay	[PMID: 14640511]
RPMI-8226	IC₅₀	16.6 μM Compound: 3	Growth inhibition of human RPMI8226 cells Growth inhibition of human RPMI8226 cells	[PMID: 18164197]
SGC-7901	IC₅₀	0.63 μM Compound: 1	Cytotoxic activity against human SGC7901 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human SGC7901 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
SW982	IC₅₀	1.28 μM Compound: B, triterpene quinine methide	Cytotoxicity against human SW982 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SW982 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23395966]
T cell line	CC₅₀	2.4 μM Compound: 1a	Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32822186]
T cell line	IC₅₀	1202 nM Compound: 1a	Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay	[PMID: 32822186]
U-87MG ATCC	ED₅₀	0.17 μg/mL Compound: 7	Cytotoxicity against human U87MG cells after 3 days by SRB assay Cytotoxicity against human U87MG cells after 3 days by SRB assay	[PMID: 14640511]

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].

MedChemExpress (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].

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

Molecular Weight

464.64

Formula

C₃₀H₄₀O₄

CAS No.

1258-84-0

Appearance

Solid

Color

Orange to reddish brown

SMILES

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

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMF : 25 mg/mL (53.81 mM; Need ultrasonic)

DMSO : 20 mg/mL (43.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.81%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (254 KB) HNMR (276 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. King AR, et al. Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem Biol. 2009 Oct 30;16(10):1045-52. [Content Brief]

[2]. Deng Q, et al. Pristimerin inhibits angiogenesis in adjuvant-induced arthritic rats by suppressing VEGFR2 signaling pathways. Int Immunopharmacol. 2015 Dec;29(2):302-13. [Content Brief]

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	[1]. King AR, et al. Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem Biol. 2009 Oct 30;16(10):1045-52. [Content Brief] [2]. Deng Q, et al. Pristimerin inhibits angiogenesis in adjuvant-induced arthritic rats by suppressing VEGFR2 signaling pathways. Int Immunopharmacol. 2015 Dec;29(2):302-13. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / DMF	1 mM	2.1522 mL	10.7610 mL	21.5220 mL	53.8051 mL
	5 mM	0.4304 mL	2.1522 mL	4.3044 mL	10.7610 mL
	10 mM	0.2152 mL	1.0761 mL	2.1522 mL	5.3805 mL
	15 mM	0.1435 mL	0.7174 mL	1.4348 mL	3.5870 mL
	20 mM	0.1076 mL	0.5381 mL	1.0761 mL	2.6903 mL
	25 mM	0.0861 mL	0.4304 mL	0.8609 mL	2.1522 mL
	30 mM	0.0717 mL	0.3587 mL	0.7174 mL	1.7935 mL
	40 mM	0.0538 mL	0.2690 mL	0.5381 mL	1.3451 mL
DMF	50 mM	0.0430 mL	0.2152 mL	0.4304 mL	1.0761 mL

Pristimerin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pristimerin1258-84-0Celastrol methyl esterBacterialInhibitorinhibitorinhibit

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Pristimerin (Synonyms: Celastrol methyl ester)

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Other Forms of Pristimerin:

Pristimerin Related Antibodies

7 Publications Citing Use of MCE Pristimerin

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Biological Activity

Protocol

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References

Customer Review

Pristimerin Related Antibodies

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Complete Stock Solution Preparation Table

Pristimerin Related Classifications

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