ADX-102 (NS-2)
- Product Name
- ADX-102 (NS-2)
- CAS No.
- 916056-79-6
- Chemical Name
- ADX-102 (NS-2)
- Synonyms
- Reproxzlap;Reproxalap;ADX-102 (NS-2);ADX-102 (Reproxalap;Reproxalap (ADX-102);Reproxalap, 10 mM in DMSO;2-(3-Amino-6-chloroquinolin-2-yl)propan-2-ol;2-Quinolinemethanol,3-amino-6-chloro-α,α-dimethyl-;2-Quinolinemethanol, 3-amino-6-chloro-α,α-dimethyl-;Inhibitor,NS 2,Reproxalap,ADX 102,ADX102,inhibit,NS2
- CBNumber
- CB93358334
- Molecular Formula
- C12H13ClN2O
- Formula Weight
- 236.7
- MOL File
- 916056-79-6.mol
ADX-102 (NS-2) Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- A1328056
- Product name
- 2-(3-Amino-6-chloroquinolin-2-yl)propan-2-ol
- Purity
- 98%
- Packaging
- 25mg
- Price
- $165
- Updated
- 2021/12/16
- Product number
- A1328056
- Product name
- 2-(3-Amino-6-chloroquinolin-2-yl)propan-2-ol
- Purity
- 98%
- Packaging
- 50mg
- Price
- $248
- Updated
- 2021/12/16
- Product number
- A1328056
- Product name
- 2-(3-Amino-6-chloroquinolin-2-yl)propan-2-ol
- Purity
- 98%
- Packaging
- 100mg
- Price
- $345
- Updated
- 2021/12/16
- Product number
- A1328056
- Product name
- 2-(3-Amino-6-chloroquinolin-2-yl)propan-2-ol
- Purity
- 98%
- Packaging
- 250mg
- Price
- $572
- Updated
- 2021/12/16
- Product number
- DC11097
- Product name
- ADX-102(Reproxalap;NS-2)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $650
- Updated
- 2021/12/16
ADX-102 (NS-2) Chemical Properties,Usage,Production
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.
ADX-102 (NS-2) Preparation Products And Raw materials
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