AS2717638

Key Product Details

Product Description

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.

Product Specifications for AS2717638

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Medeiros Geraldo Role of lysophosphatidic acid and its receptors in health and disease: novel therapeutic strategies. Signal Transduct.Target.Ther. 2021 PMID: 33526777
• Murai Analgesic effects of novel lysophosphatidic acid receptor 5 antagonist AS2717638 in rodents. Neuropharmacology 2017 PMID: 28859883
• Joshi 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. 2021 PMID: 34445223
• Tsukahara LPA5 signaling is involved in multiple sclerosis-mediated neuropathic pain in the cuprizone mouse model. J.Pharmacol.Sci. 2018 PMID: 29409686
• Joshi 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 2022 PMID: 35406635

Product Documents for AS2717638