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Biochem/physiol Actions
HTS01037 is a selective, high-affinity fatty acid-binding protein FABP4 (AFABP; aP2) antagonist (aP2 Ki = 0.67 μM; EFABP/HF/IFABP/LFABP Ki = 3.40/9.07/6.57/8.17 μM) that targets aP2 long-chain fatty acid-binding site. HTS01037 is shown to downregulate basal and fatty acid-stimulated LTC4 levels in primary murine peritoneal macrophages (0.2-20 μM), upregulate murine macrophage RAW 264.7 intracellular free fatty acids and uncoupling protein 2 (UCP2) mRNA levels (30 μM), as well as suppress PPARγ target genes expression in IL-4 polarized human primary macrophages (10-25 μM).
Selective, high-affinity fatty acid-binding protein FABP4 (AFABP; aP2) antagonist that blocks aP2-mediated responses in human and murine macrophages.
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | [s]1c(cc(c1C(=O)OC)NC(=O)C=CC(=O)O)c2[s]ccc2 |
| InChI | 1S/C14H11NO5S2/c1-20-14(19)13-8(15-11(16)4-5-12(17)18)7-10(22-13)9-3-2-6-21-9/h2-7H,1H3,(H,15,16)(H,17,18) |
| InChI key | GJODSFZNKNHKML-UHFFFAOYSA-N |
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