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Submit ReviewAS2717638
说明： Selective, brain penetrant LPA5 antagonist
化学名： 6,7-Dimethoxy-2-(5-methyl-1,2-benzisoxazol-3-yl)-4-(1-piperidinylcarbonyl)-1(2H)-isoquinolinone
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for AS2717638
| 分子量 | 447.48 |
| 公式 | C25H25N3O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for AS2717638
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 4.47 | 10 |
制备储备液 for AS2717638
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for AS2717638
参考文献 for AS2717638
参考文献是支持产品生物活性的出版物。
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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关键词: 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
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