ADX-102 (NS-2)
ADX-102 (NS-2) Basic information
- Product Name:
- ADX-102 (NS-2)
- Synonyms:
-
- ADX-102 (NS-2)
- Reproxalap
- 2-Quinolinemethanol, 3-amino-6-chloro-α,α-dimethyl-
- ADX-102 (Reproxalap
- 2-(3-Amino-6-chloroquinolin-2-yl)propan-2-ol
- Reproxzlap
- Reproxalap (ADX-102)
- Inhibitor,NS 2,Reproxalap,ADX 102,ADX102,inhibit,NS2
- CAS:
- 916056-79-6
- MF:
- C12H13ClN2O
- MW:
- 236.7
- Mol File:
- 916056-79-6.mol
ADX-102 (NS-2) 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
ADX-102 (NS-2) Usage And Synthesis
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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