| Identification | Back Directory | [Name]
AS2717638 | [CAS]
2148339-28-8 | [Synonyms]
AS2717638
1(2H)-Isoquinolinone, 6,7-dimethoxy-2-(5-methyl-1,2-benzisoxazol-3-yl)-4-(1-piperidinylcarbonyl)- | [Molecular Formula]
C25H25N3O5 | [MDL Number]
MFCD31813748 | [MOL File]
2148339-28-8.mol | [Molecular Weight]
447.48 |
| Chemical Properties | Back Directory | [Boiling point ]
712.5±60.0 °C(Predicted) | [density ]
1.321±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 2 mg/ml; DMSO: 2 mg/ml | [form ]
A solid | [pka]
-1.17±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
Orally activepotent and selective lysophosphatidic acid (LPA) receptor LPAR5 (LPA5) antagonist with analgesic efficacy in vivo.
AS2717638 is an orally activepotent and selective lysophosphatidic acid (LPA) receptor LPAR5 (LPA5) antagonist (h/m/r LPA5 Ki = 9.1/7.3/16 nM) th at blocks LPA-induced activation of human LPA5-expressing cells (cAMP accumulation IC50 = 38 nM)but not LPA1LPA2 or LPA3 transfectants (Ca2+ mobilization IC50 >10 μM) and displays much reduced or little affinity toward 20 other receptors and channels. AS2717638 exhibits analgesic efficacy in mice (10 & 30 mg/kg p.o. against allodynia caused by 10 ng PGE2300 ng PGF2αor 3 ng AMPA per mouse via i.t.) and rats (10 mg/kg p.o. against mechanical allodyniathermal hyperalgesia and adjuvant-induced inflammatory pain) in vivo. | [storage]
Store at -20°C |
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DC Chemicals
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http://m.is0513.com/ShowSupplierProductsList927327/0.htm |
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www.sangon.com |
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MedChemExpress
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www.medchemexpress.com |
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