Pristimerin
Based on 8 publication(s) in Google Scholar
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.
- Purity: 99.81%
- CAS No.: 1258-84-0
- Formula: C30H40O4
- Molecular Weight:464.64
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Pristimerin
More- Phytomedicine. 2021 Jan;80:153399. [Abstract]
- Cell Death Discov. 2025 Dec 8. [Abstract]
- Drug Des Devel Ther. 2024 Nov 27:18:5445-5459. [Abstract]
- Drug Des Devel Ther. 2020 Oct 9;14:4189-4203. [Abstract]
- Int Immunopharmacol. 2021 May:94:107491. [Abstract]
- Mol Med Rep. 2025 Jun;31(6):153. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2026 May 29. [Abstract]
- Vet Microbiol. 2025 Sep 15:310:110730. [Abstract]
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WB
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Cell Imaging/Staining
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RT-PCR
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
Biological Activity
IC50: 93 nM (MGL)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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
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[PMID: 14640511] |
| 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/ptx-10 | ED50 |
0.076 μg/mL
Compound: 7
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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
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[PMID: 14640511] |
| A549 | ED50 |
0.31 μg/mL
Compound: 7
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Cytotoxicity against human A549 cells after 3 days by SRB assay
Cytotoxicity against human A549 cells after 3 days by SRB assay
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[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
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[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
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[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
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Cytotoxicity against human HCT8 cells after 3 days by SRB assay
Cytotoxicity against human HCT8 cells after 3 days by SRB assay
|
[PMID: 14640511] |
| 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
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[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
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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
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[PMID: 28587825] |
| HL-60 | IC50 |
0.2 μM
Compound: 23
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Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
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[PMID: 21090801] |
| HT-29 | IC50 |
4600 ng/mL
Compound: 6
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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
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[PMID: 9644053] |
| Huh-7 | CC50 |
>6.25 μM
Compound: GNF-Pf-476
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[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
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Cytotoxicity against human KB cells by MTT assay
Cytotoxicity against human KB cells by MTT assay
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[PMID: 7714534] |
| KB | IC50 |
0.9 μM
Compound: 1a
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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
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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
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[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
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[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
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[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
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[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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1258-84-0
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Appearance Solid
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Molecular Weight 464.64
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Formula C30H40O4
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Color Orange to reddish brown
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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
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Synonyms
Celastrol methyl ester
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Effect of pristimerin on apoptosis through activation of ROS/ endoplasmic reticulum (ER) stress-mediated noxa in colorectal cancer. [Abstract]2021 Jan;80:153399. PMID: 33202325 -
Cell Death Discov
The glycolytic enzyme PFKFB3 alleviates DNA damage and chondrocyte senescence in osteoarthritis. [Abstract]2025 Dec 8. PMID: 41360766
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).
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Drug Des Devel Ther
The Therapeutic Potential of Pristimerin in Osteoarthritis: Mechanistic Insights from in vitro and in vivo Studies. [Abstract]2024 Nov 27:18:5445-5459. PMID: 39628956
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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Drug Des Devel Ther
Pristimerin Inhibits Osteoclast Differentiation and Bone Resorption in vitro and Prevents Ovariectomy-Induced Bone Loss in vivo. [Abstract]2020 Oct 9;14:4189-4203. PMID: 33116407 -
Int Immunopharmacol
Pristimerin reduces dextran sulfate sodium-induced colitis in mice by inhibiting microRNA-155. [Abstract]2021 May:94:107491. PMID: 33770552 -
Mol Med Rep
Pristimerin ameliorates colitis‑induced intestinal mucosal injury by inhibiting intestinal epithelial necroptosis. [Abstract]2025 Jun;31(6):153. PMID: 40211716 -
Naunyn Schmiedebergs Arch Pharmacol
2026 May 29. PMID: 42209734 -
Vet Microbiol
Identification and evaluation of Nordihydroguaiaretic acid (NDGA) as an active traditional Chinese medicine compound inhibiting the 3C-like protease of feline infectious peritonitis virus. [Abstract]2025 Sep 15:310:110730. PMID: 40976146
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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]
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.
| 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 |