| Identification | Back Directory | [Name]
4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]- | [CAS]
923417-09-8 | [Synonyms]
VU533
4-Piperidinecarboxamide, N-(4,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-
N-(4,7-Dimethylbenzo[d]thiazol-2-yl)-1-((4-fluorophenyl)sulfonyl)piperidine-4-carboxamide , VU533 | [Molecular Formula]
C21H22FN3O3S2 | [MOL File]
923417-09-8.mol | [Molecular Weight]
447.55 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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-targetingreversiblepotent 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)reversiblepotent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D activator (mouse EC50/Emax = 0.30 μM/2.6-foldhuman EC50/Emax = 0.2 μM/1.9-foldusing respective recombinant NAPE-PLD) th at targets an allosteric site distinct from th at of PEDCAor LEI-401showing 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 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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