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Submit ReviewAS2717638
Description: Selective, brain penetrant LPA5 antagonist
Chemical Name: 6,7-Dimethoxy-2-(5-methyl-1,2-benzisoxazol-3-yl)-4-(1-piperidinylcarbonyl)-1(2H)-isoquinolinone
Purity: ≥98% (HPLC)
Biological Activity for AS2717638
AS2717638 is a potent LPA5 receptor antagonist (IC50 = 38 nM in BV-2 microglia cells). It is selective for LPA5 over LPA1, LPA2, and LPA3. It inhibits LPA-mediated pro-inflammatory transcription factor phosphorylation. In vivo, AS2717638 inhibits LPA5 agonist-induced allodynia in mice. It also exhibits analgesic effects against both neuropathic and inflammatory pain in rodent models. Orally bioavailable and brain penetrant.
Technical Data for AS2717638
| M. Wt | 447.48 |
| Formula | C25H25N3O5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2148339-28-8 |
| PubChem ID | 137333453 |
| InChI Key | QRMYHYZQUGJBBX-UHFFFAOYSA-N |
| Smiles | O=C1C=2C=C(OC)C(OC)=CC2C(=CN1C3=NOC=4C=CC(=CC43)C)C(=O)N5CCCCC5 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AS2717638
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.47 | 10 |
Preparing Stock Solutions for AS2717638
The following data is based on the product molecular weight 447.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 22.35 mL | 111.74 mL | 223.47 mL |
| 0.5 mM | 4.47 mL | 22.35 mL | 44.69 mL |
| 1 mM | 2.23 mL | 11.17 mL | 22.35 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.47 mL |
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Product Datasheets for AS2717638
References for AS2717638
References are publications that support the biological activity of the product.
Joshi et al (2022) Lysophosphatidic acid receptor 5 (LPA5) knockout ameliorates the neuroinflammatory response in vivo and modifies the inflammatory and metabolic landscape of primary microglia in vitro. Cells 11 1071 PMID: 35406635
Joshi et al (2021) Inhibition of autotaxin and lysophosphatidic acid receptor 5 attenuates neuroinflammation in LPS-activated BV-2 microglia and a mouse endotoxemia model. Int.J.Mol.Sci. 22 8519 PMID: 34445223
Tsukahara et al (2018) LPA5 signaling is involved in multiple sclerosis-mediated neuropathic pain in the cuprizone mouse model. J.Pharmacol.Sci. 136 93 PMID: 29409686
Murai et al (2017) Analgesic effects of novel lysophosphatidic acid receptor 5 antagonist AS2717638 in rodents. Neuropharmacology 126 97 PMID: 28859883
Medeiros Geraldo et al (2021) Role of lysophosphatidic acid and its receptors in health and disease: novel therapeutic strategies. Signal Transduct.Target.Ther. 6 45 PMID: 33526777
If you know of a relevant reference for AS2717638, please let us know.
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Keywords: AS2717638, AS2717638 supplier, LPA, LPA5, lysophosphatidic, acid, receptors, antagonists, antagonism, neuroinflammation, in, vivo, orally, bioavailable, brain, penetrant, potent, selective, Lysophosphatidic, Acid, Receptors, 7730, Tocris Bioscience
Citations for AS2717638
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