AS2717638
CAS No. : 2148339-28-8
| Size | Price | Stock |
|---|---|---|
| 5mg | $155 | In-stock |
| 10mg | $255 | In-stock |
| 25mg | $510 | In-stock |
| 50mg | $820 | In-stock |
| 100mg | $1300 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-114379 |
| M.Wt: | 447.48 |
| Formula: | C25H25N3O5 |
| Purity: | >98 % |
| Solubility: | DMSO : 60 mg/mL (ultrasonic) |
AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC50 value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases[1][2].
IC50 & Target:IC50: 38 nM (hLPA5)[1].
In Vitro:AS2717638 (0.038 μM; 20 min) inhibits LPA-induced cAMP accumulation in the cAMP accumulation assay using CHO cells expressing human LPA5[2].
AS2717638 (0.1 μM, 1 μM; 24 h) has no effect on MTT reduction in BV-2 cells, and the cell viability is not significantly affected; at 10 μM (24 h), the cell viability is reduced by 50%[2].
AS2717638 (0.1-1 μM; 2-24 h) inhibits the phosphorylation of STAT1, p65, and c-Jun in LPS-stimulated BV-2 cells. AS2717638 reduces the expression of TLR4 and COX2, and decreases NO production in LPS-stimulated BV-2 cells[2].
AS2717638 (0.1-1 μM; 2-24 h) reduces the secretion of cytokines and chemokines such as TNFα, IL-6, CXCL10, CXCL2, and CCL5 in the supernatants of LPS-stimulated BV-2 cell cultures[2].
In Vivo:AS2717638 (3-30 mg/kg; oral administration; 1 h before the experiment; single dose) inhibits allodynia in mouse models of allodynia induced by LPA or GGPP[1].
AS2717638 (10-30 mg/kg; oral administration; 1 h before the experiment; single dose) alleviates allodynia in mouse models of allodynia induced by PGE2, PGF2α, or AMPA[1].
AS2717638 (10 mg/kg; oral administration; 2 h before the experiment; single dose) ameliorates static mechanical allodynia and thermal hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI)[1].
AS2717638 (10 mg/kg; oral administration; 2 h before the experiment; single dose) improves hind paw weight - bearing ability in a rat model of inflammatory pain induced by adjuvant[1].
AS2717638 (10 mg/kg; oral administration; before the experiment; single dose) reduces LPS (HY-D1056)-induced iNOS, TNFα, IL-6, and CXCL2 mRNA expression, improves the expression of neuroinflammation - related proteins, and reduces peripheral cytokine concentrations in a mouse endotoxemia model[2].
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