| Identification | Back Directory | [Name]
ADX-102 (NS-2) | [CAS]
916056-79-6 | [Synonyms]
Reproxalap
ADX-102 (NS-2)
ADX-102 (Reproxalap
2-Quinolinemethanol, 3-amino-6-chloro-α,α-dimethyl- | [Molecular Formula]
C12H13ClN2O | [MDL Number]
MFCD28502442 | [MOL File]
916056-79-6.mol | [Molecular Weight]
236.7 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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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