ChemicalBook CAS DataBase List 916056-79-6

916056-79-6

Name	ADX-102 (NS-2)
CAS	916056-79-6
Molecular Formula	C12H13ClN2O
MDL Number	MFCD28502442
Molecular Weight	236.7
MOL File	916056-79-6.mol

Chemical Properties

Boiling point	410.5±40.0 °C(Predicted)
density	1.324±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : 100 mg/mL (422.48 mM; Need ultrasonic)
form	Solid
pka	13.07±0.29(Predicted)
color	Light yellow to yellow
InChI	InChI=1S/C12H13ClN2O/c1-12(2,16)11-9(14)6-7-5-8(13)3-4-10(7)15-11/h3-6,16H,14H2,1-2H3
InChIKey	GUHFUVLKYSQIOQ-UHFFFAOYSA-N
SMILES	CC(C1=C(N)C=C2C(=N1)C=CC(Cl)=C2)(O)C

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338

Hazard Information

Uses

Reproxalap (ADX-102) is an active aldehyde sequestering agent. Reproxalap reduces the PKCα activity. Reproxalap blocks caspase 3/7 activation. Reproxalap protects cells from the cytotoxicity of C18:0-al. Reproxalap has anti-inflammatory and pain-relieving effects. Reproxalap is used in studies of dry eye, allergic conjunctivitis, and non-infectious anterior uveitis[1][2][3][4][5].

in vivo

Reproxalap (30-100 mg/kg, once or twice a day) shows a dose-dependent reduction in pain-related behaviors in acute pain models^[3].
Reproxalap (10 mg/kg, intraperitoneal injection, single dose) significantly reduces the formation of N-retinyl-phosphatidylethanolamine (A2E) in the retinas of mice with macular degeneration^[5].
Reproxalap (25-50 μg, IVT, injected in five doses after LPS (HY-D1056) induction) can improve eye scores in uveitis rats^[5].

Animal Model:	Carrageenaninduced and Complete Freund’s Adjuvant (CFA)-induced models in mice^[3]
Dosage:	30, 100 mg/kg; once a day or twice a day
Administration:
Result:	Was effective in thermal hyperalgesia in the CFA-induced model at both 100 mg/kg QD and BID doses; in the carrageenan-induced model, and was effective at 30 mg/kg BID and 100 mg/kg BID doses. Was effective in mechanical allodynia only in the CFA-induced model at a 100 mg/kg BID dose; in the carrageenan-induced model, was not effective. Had a mild effect on swelling in the CFA-induced model at 30 mg/kg BID and 100 mg/kg BID doses; in the carrageenan-induced model, had a mild effect at a 100 mg/kg QD dose.

Animal Model:	A mouse knockout model (abcr-/-) of macular degeneration (MD) ^[5]
Dosage:	10 mg/kg; single dose
Administration:	Intraperitoneal injection (i.p.)
Result:	Reduced the formation of N-retinylidene-N-retinylethanolamine (A2E) in the retina by 71% without affecting dark adaptation or body weight.

Animal Model:	A rat model of lipopolysaccharide (LPS)-induced uveitis^[5]
Dosage:	10 mg/kg 50 μg at hours 1, 3, 7, 10 and 17, after LPS induction, or injection 25 μg at 1 hour after LPS induction
Administration:	Intravitreal (IVT)
Result:	Improved the eye examination scores, enhancing the retinal-choroidal ratings.

IC 50

PKCα; Caspase 3; Caspase-7

References

[1] Ochoa CA, et al. Aldehyde Trapping by ADX-102 Is Protective against Cigarette Smoke and Alcohol Mediated Lung Cell Injury. Biomolecules. 2022 Mar 2;12(3):393. DOI:10.3390/biom12030393
[2] Rizzo WB, et al. Sj?gren-Larsson syndrome: A biochemical rationale for using aldehyde-reactive therapeutic agents. Mol Genet Metab Rep. 2021 Dec 23;30:100839. DOI:10.1016/j.ymgmr.2021.100839
[3] Susan Macdonald, et al. ADX-102, a novel aldehyde trap, reduces nociceptive behavior in mouse models of carrageenan and CFA induced pain.
[4] Reproxalap Phase 2b Dry Eye Disease Results.
[5] Susan G. Macdonald, Ph.D., et al. Novel Small Molecule Aldehyde Sequestering Agents Demonstrate Broad Therapeutic Potential for Ocular Inflammation.

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