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AS2717638

Catalog #: 7730 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7730/10
AS2717638 | CAS No. 2148339-28-8 | LPAR5/LPA5/GPR92
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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%

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Biological Activity

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

M.Wt:
447.48
Formula:
C25H25N3O5
Solubility:
Soluble to 10 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2148339-28-8

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.

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