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Merck
CN

SML3738

Sigma-Aldrich

AS2717638

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C25H25N3O5
CAS Number:
2148339-28-8
Molecular Weight:
447.48
MDL number:
MFCD31813748

Key Documents

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Quality Level

100

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000394043
0000394042
0000382541
0000382541
0000394042

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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
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
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
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
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)

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