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AS2717638
- Soluble in DMSO and EtOH
- MF: C25H25N3O5
- MW: 447.48
Description
AS2717638 is a highly potent, selective, orally active, and brain-penetrant lysophosphatidic acid (LPA) receptor 5 antagonist (IC50 value of 0.038 μM). AS2717638 blunted LPA-induced phosphorylation of STAT1 and STAT3, p65, and c-Jun and consequently reduced the secretion of pro-inflammatory cyto-/chemokines (IL-6, TNFα, IL-1β, CXCL10, CXCL2, and CCL5) at non-toxic concentrations. Moreover, AS271763 modulated the expression of intracellular (COX-2 and Arg1) and plasma membrane-located (CD40, CD86, and CD206) polarization markers and attenuated the neurotoxic potential of LPA-activated BV-2 cell-conditioned medium towards CATH.a neurons.
More Information
| Parent CAS No. | 2148339-28-8 |
|---|---|
| Chemical Name | 6,7-Dimethoxy-2-(5-methylbenzo[d]isoxazol-3-yl)-4-(piperidine-1-carbonyl)isoquinolin-1(2H)-one |
| SMILES | C1(OC)C=C2C(=O)N(C3=NOC4C=CC(C)=CC3=4)C=C(C(N3CCCCC3)=O)C2=CC=1OC |
| MFCD | N.A. |
| InChi | InChI=1S/C25H25N3O5/c1-15-7-8-20-18(11-15)23(26-33-20)28-14-19(24(29)27-9-5-4-6-10-27)16-12-21(31-2)22(32-3)13-17(16)25(28)30/h7-8,11-14H,4-6,9-10H2,1-3H3 |
| InChiKey | QRMYHYZQUGJBBX-UHFFFAOYSA-N |
| CID | 137333453 |
| Short Description | LPA receptor 5 antagonist |
References
- N Murai et al. Analgesic effects of novel lysophosphatidic acid receptor 5 antagonist AS2717638 in rodents. Neuropharmacology. 2017 Nov;126:97-107.
- I Plastira et al. Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells. Front Cell Neurosci. 2019 Nov 29;13:531.
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