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Pristimerin (Celastrol-methylether; UNII-28ZK7PR57S) is a naturally occurring triterpenoid, acting as a reversible monoacylglycerol lipase (MGL) inhibitor (IC50 = 93 nM) with antitumor activity. It induces caspase-dependent apoptosis by inhibiting the chymotrypsin-like activity of the proteasome.
| ln Vitro |
Pristimerin has been shown to suppress the activity of both pure and non-purified MGL (transfected HeLa cell cell lysates) at an IC50 of 93±8 nM and 398±68 nM, respectively. Pristimerin works as a fast, reversible, and non-competitive inhibitor of MGL. By forming a polar contact with a regulating cysteine, perhaps Cys208, prismerin's binding to MGL may be enhanced[1]. Pristimerin has a dose- and time-dependent effect on the viability of HFLS-RA and HUVEC cells. Pristimerin lowers the autophosphorylation of VEGFR2 caused by VEGF and lessens the activation of the VEGFR2-mediated signaling pathway generated by VEGF [2].
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| ln Vivo |
Tumor angiogenesis and inflammation are both inhibited by pramimerin. Pristimerin considerably lowers the expression of pro-angiogenic factors in sera, such as TNF-α, Ang-1, and MMP-9, and significantly reduces vessel density in the synovial membrane tissues of inflamed joints[2].
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| References |
[1]. King AR, et al. Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem Biol. 2009 Oct 30;16(10):1045-52.
[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 |
| Molecular Formula |
C30H40O4
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|---|---|
| Molecular Weight |
464.65
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| Exact Mass |
464.2927
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| CAS # |
1258-84-0
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| Related CAS # |
Celastrol;34157-83-0
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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 |
UNII-28ZK7PR57S Celastrol-methylether Pristimerin
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMF : 25 mg/mL (~53.81 mM)
DMSO : ~20 mg/mL (~43.04 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1522 mL | 10.7608 mL | 21.5216 mL | |
| 5 mM | 0.4304 mL | 2.1522 mL | 4.3043 mL | |
| 10 mM | 0.2152 mL | 1.0761 mL | 2.1522 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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