2079895-60-4

Name	4H-Pyrrolo[3,4-c][1,6]naphthyridin-4-one, 2-(5-benzofuranylsulfonyl)-1,2,3,3a,5,9b-hexahydro-5-methyl-, (3aS,9bS)-
CAS	2079895-60-4
Molecular Formula	C19H17N3O4S
Molecular Weight	383.42
MOL File	2079895-60-4.mol

Synonyms

4H-Pyrrolo[3,4-c][1,6]naphthyridin-4-one, 2-(5-benzofuranylsulfonyl)-1,2,3,3a,5,9b-hexahydro-5-methyl-, (3aS,9bS)-

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Chemical Properties

Boiling point	645.5±65.0 °C(Predicted)
density	1.438±0.06 g/cm3(Predicted)
pka	6.11±0.20(Predicted)

Hazard Information

Description

AM1488 is a Potent and Efficacious Potentiator of Glycine Receptor.

Uses

AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC50=0.45 μM)[1][2].

in vivo

AM-1488 (oral gavage; 20 mg/kg; once) treatment significantly reverse mechanical allodynia induced by nerve injury in a mouse model of neuropathic pain, without being confounded by sedation or motor side effects^[1].

Animal Model:	Mouse model of spared nerve injury (SNI)^[1]
Dosage:	20 mg/kg
Administration:	Oral gavage; 20 mg/kg; once
Result:	Produced a significant 94% reversal of tactile allodynia, and the unbound brain concentration was 2.8- and 1.6-fold higher than the mouse GlyRα1 and GlyRα3 EC₅₀ values, respectively.

Animal Model:	Naive mice^[1]
Dosage:	20 mg/kg
Administration:	Oral gavage; 20 mg/kg; once
Result:	Showed not significantly different from mice treated with vehicle.

References

[1] Xin Huang, et al. Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators. Nat Struct Mol Biol. 2017 Feb;24(2):108-113. DOI:10.1038/nsmb.3329
[2] Howard Bregman, et al. The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors. J Med Chem. 2017 Feb 9;60(3):1105-1125. DOI:10.1021/acs.jmedchem.6b01496

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TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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