AS2717638

Name: AS2717638
Brand: Tocris Bioscience
SKU: 7730

Tocris Bioscience, part of Bio-Techne | Catalog # 7730

COA / SDS

Selective, brain penetrant LPA5 antagonist

Key Product Details

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)
Molecular Weight:	447.48

View Full Technical Details for AS2717638

Technical Data
Citations

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 for AS2717638

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for AS2717638

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