1-Piperazinecarboxylic acid, 4-[[2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester
ABX-1431
CAS: 1446817-84-0
Molecular Formula: C20H22F9N3O2
1-Piperazinecarboxylic acid, 4-[[2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester - Names and Identifiers
1-Piperazinecarboxylic acid, 4-[[2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester - Physico-chemical Properties
| Molecular Formula | C20H22F9N3O2 |
| Molar Mass | 507.39 |
| Solubility | Soluble in DMSO (>25 mg/ml) |
| Appearance | solid |
| Color | White |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| In vitro study | ABX-1431 is a potent human MGLL inhibitor with an IC50 of 0.014 μm and is more than 100 times more selective for MGLL than for ABHD6 and more than 200 times more selective for PLA2G7. Treatment of PC3 cells with ABX-1431 for 30 minutes ABX-1431 resulted in inhibition of intracellular MGLL activity with an IC50 of 0.0022 μm. ABX-1431 inhibits MGLL by formylating the nucleophilic site Ser122 in the MGLL catalytic subunit. |
| In vivo study | ABX-1431 pharmacokinetic studies in rats and dogs revealed low to moderate systemic clearance, moderate volume of distribution, and high oral bioavailability of ABX-1431 (Rat 64%, dog 57%). ABX-1431 is stable in human and dog plasma, but not in rat plasma. ABX-1431 is a potent, selective inhibitor of MGLL in the brain in rats and mice. In the mouse brain, ABX-1431 inhibiting the activity of mg11, ED50 was 0.5-1.4 mg/kg (po), increasing intracerebral 2-AG levels in a concentration-dependent manner. Using rat inflammatory pain model to test the pharmacological effects of ABX-1431: in formalin paw test, use the concentration that can nearly completely inhibit MGLL and maximize the level of 2-AG, ABX-1431 has an effective analgesic effect. |
1-Piperazinecarboxylic acid, 4-[[2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.971 ml | 9.854 ml | 19.709 ml |
| 5 mM | 0.394 ml | 1.971 ml | 3.942 ml |
| 10 mM | 0.197 ml | 0.985 ml | 1.971 ml |
| 5 mM | 0.039 ml | 0.197 ml | 0.394 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: ABX-1431 Visit Supplier Webpage Request for quotationCAS: 1446817-84-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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