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| | 4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- Basic information |
| Product Name: | 4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- | | Synonyms: | 4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-;VU533;N-(4,7-Dimethylbenzo[d]thiazol-2-yl)-1-((4-fluorophenyl)sulfonyl)piperidine-4-carboxamide , VU533;Nape-Pld activator;N-(4,7-dimethylbenzo[d]thiazol-2-yl)-1-((4-fluorophenyl)sulfonyl)piperidine-4-carboxamide;N-(4,7-Dimethylbenzo[d]thiazol-2-yl)-1-((4-fluorophenyChemicalbookl)sulfonyl)piperidine-4-carboxamide,VU53;N-(4,7-Dimethylbenzo[d]thiazol-2-yl)-1-((4-fluorophenyChemicalbookl)sulfonyl)piperidine-4-carboxamide,VU533 | | CAS: | 923417-09-8 | | MF: | C21H22FN3O3S2 | | MW: | 447.55 | | EINECS: | | | Product Categories: | | | Mol File: | 923417-09-8.mol | ![4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- Structure](CAS/20200331/GIF/923417-09-8.gif) |
| | 4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- Chemical Properties |
| density | 1.412±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 2mg/mL, clear (Warmed) | | form | Solid | | pka | 10.39±0.70(Predicted) | | color | White to off-white | | SMILES | O=C(C1CCN(S(=O)(C2=CC=C(C=C2)F)=O)CC1)NC3=NC4=C(C)C=CC(C)=C4S3 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral |
| | 4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- Usage And Synthesis |
| Uses | APE-PLD (VU533) activator is a potent NAPE-PLD activator with an EC50 value of 0.30 μM. NAPE-PLD activator (VU533) can enhance NAPE-PLD activity and increase efferocytosis by macrophages. NAPE-PLD activator (VU533) can be used for cardiometabolic diseases research[1]. | | Biological Activity | Allosteric site-targeting, reversible, potent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D (NAPE-PLD) activator.
VU533 is a non-cytotoxic (up to 30 μM in murine RAW264.7 and human HepG2 cultures), reversible, potent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D activator (mouse EC50/Emax = 0.30 μM/2.6-fold, human EC50/Emax = 0.2 μM/1.9-fold, using respective recombinant NAPE-PLD) th at targets an allosteric site distinct from th at of PE, DCA, or LEI-401, showing only little potency toward FAAH and sEH. VU533 enhances murine BMDMs efferocytosis (by 1.53-fold with 6h 10 μM pretreatment) by activating cellular NAPE-PLD activity (EC50/Emax = 2.5 μM/2.2-fold in RAW264.7 and 3.0 μM/1.6-fold in HepG2). | | IC 50 | PLD1: 0.3 μM (EC50) | | References | [1] Zarrow JE, et al. Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages. ACS Chem Biol. 2023 Aug 18;18(8):1891-1904. DOI:10.1021/acschembio.3c00401 |
| | 4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- Preparation Products And Raw materials |
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