SML3738
AS2717638
≥98% (HPLC)
别名:
6,7-Dimethoxy-2-(5-methyl-1,2-benzisoxazol-3-yl)-4-(1-piperidinylcarbonyl)-1(2H )-isoquinolinone, 6,7-Dimethoxy-2-(5-methyl-1,2-benzoxazol-3-yl)-4-(piperidin-1-ylcarbonyl)isoquinolin-1(2H)-one, AS 2717638, AS-2717638
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关于此项目
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
SMILES string
O=C1C2=C(C(C(N3CCCCC3)=O)=CN1C4=NOC5=C4C=C(C)C=C5)C=C(OC)C(OC)=C2
InChI
1S/C25H25N3O5/c1-15-7-8-20-18(11-15)23(26-33-20)28-14-19(24(29)27-9-5-4-6-10-27)16-12-21(31-2)22(32-3)13-17(16)25(28)30/h7-8,11-14H,4-6,9-10H2,1-3H3
InChI key
QRMYHYZQUGJBBX-UHFFFAOYSA-N
Biochem/physiol Actions
Orally active, potent and selective lysophosphatidic acid (LPA) receptor LPAR5 (LPA5) antagonist with analgesic efficacy in vivo.
AS2717638 is an orally active, potent and selective lysophosphatidic acid (LPA) receptor LPAR5 (LPA5) antagonist (h/m/r LPA5 Ki = 9.1/7.3/16 nM) that blocks LPA-induced activation of human LPA5-expressing cells (cAMP accumulation IC50 = 38 nM), but not LPA1, LPA2 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 PGE2, 300 ng PGF2α, or 3 ng AMPA per mouse via i.t.) and rats (10 mg/kg p.o. against mechanical allodynia, thermal hyperalgesia and adjuvant-induced inflammatory pain) in vivo.
AS2717638 is an orally active, potent and selective lysophosphatidic acid (LPA) receptor LPAR5 (LPA5) antagonist (h/m/r LPA5 Ki = 9.1/7.3/16 nM) that blocks LPA-induced activation of human LPA5-expressing cells (cAMP accumulation IC50 = 38 nM), but not LPA1, LPA2 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 PGE2, 300 ng PGF2α, or 3 ng AMPA per mouse via i.t.) and rats (10 mg/kg p.o. against mechanical allodynia, thermal hyperalgesia and adjuvant-induced inflammatory pain) in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Ioanna Plastira et al.
Frontiers in cellular neuroscience, 13, 531-531 (2019-12-19)
Lysophosphatidic acid (LPA) species in the extracellular environment induce downstream signaling via six different G protein-coupled receptors (LPAR1-6). These signaling cascades are essential for normal brain development and function of the nervous system. However, in response to acute or chronic
Zhongxing Liang et al.
Cells, 11(14) (2022-07-28)
Renewal of the intestinal epithelium is orchestrated by regenerative epithelial proliferation within crypts. Recent studies have shown that lysophosphatidic acid (LPA) can maintain intestinal epithelial renewal in vitro and conditional deletion of Lpar5 (Lpar5iKO) in mice ablates the intestinal epithelium
Dehui Zhang et al.
European journal of medicinal chemistry, 243, 114741-114741 (2022-09-21)
Blockade of lysophosphatidic acid receptor 5 (LPA5) by a recently reported antagonist AS2717638 (2) attenuated inflammatory and neuropathic pains, although it showed moderate in vivo efficacy and its structure-activity relationships and the ADME properties are little studied. We therefore designed
P Martin et al.
Neuropsychobiology, 18(1), 21-26 (1987-01-01)
Several investigations have suggested that a special relationship exists between thyroid function and affective disorders and/or therapeutic response to antidepressants. The present study shows that the reversal by clomipramine, desipramine, imipramine and nialamide of depressive-like behavior in rats (escape deficits
Nobuhito Murai et al.
Neuropharmacology, 126, 97-107 (2017-09-02)
Lysophosphatidic acid (LPA) is a bioactive lipid that acts via at least six G protein-coupled receptors, LPA receptors 1-6 (LPA1-6), for various physiological functions. We examined (1) whether LPA5 is involved in pain signaling in the spinal cord; and (2)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML3738-5MG | 04065272170468 |
| SML3738-25MG | 04065272170451 |
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