| Identification | Back Directory | [Name]
N-(5,7-Dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-4-piperidinecarboxamide | [CAS]
923509-20-0 | [Synonyms]
VU534
N-(5,7-Dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-4-piperidinecarboxamide | [Molecular Formula]
C21H22FN3O3S2 | [MOL File]
923509-20-0.mol | [Molecular Weight]
447.55 |
| Chemical Properties | Back Directory | [density ]
1.412±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear (Warmed) | [form ]
Solid | [pka]
10.26±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
VU534 is a NAPE-PLD activator, with an EC50 of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC50 of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study [1] . | [Biological Activity]
Allosteric site-targetingreversiblepotent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D (NAPE-PLD) activator.
VU534 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/2.1-foldhuman EC50/Emax = 0.93 μM/1.8-foldusing respective recombinant NAPE-PLD) th at targets an allosteric site distinct from th at of PEDCAor LEI-401showing only weak sEH inhibition (IC50/Emax = 1.2 μM/55%) and little potency toward FAAH. VU534 enhances murine BMDMs efferocytosis (by 1.65-fold with 6h 10 μM pretreatment) by activating cellular NAPE-PLD activity (EC50/Emax = 6.6 μM/1.6-fold in RAW264.7 and 1.5 μM/1.6-fold in HepG2). | [References]
[1] Jonah E Zarrow, et al. Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages. ACS Chem. Biol. 2023, 18, 8, 1891–1904. DOI:10.1101/2023.01.25.525554 |
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Merck KGaA
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21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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