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.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-124454 |
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| Réf. fabricant | 18777546 |
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| Nom chimique ou matériau | 6,7-Dimethoxy-2-(5-methyl-1,2-benzisoxazol-3-yl)-4-(1-piperidinylcarbonyl)-1(2 H)-isoquinolinone |
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| CAS | 2148339-28-8 |
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| Quantité | 10 mg |
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| Cible | LPAR5/LPA5/GPR92 |
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| Formule moléculaire | C<sub>25</sub>H<sub>25</sub>N<sub>3</sub>O<sub>5</sub> |
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| Pureté | 0.98 |
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