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| 500mg |
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Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal. Reproxalap is a novel small-molecule immune-modulating covalent inhibitor of RASP (reactive aldehyde species), which are elevated in ocular and systemic inflammatory disease.
| Targets |
RASP (reactive aldehyde species) sequestering agent
|
|---|---|
| ln Vitro |
ADX-102 is a novel small molecule that covalently binds aldehydes, including malondialdehyde and 4-hydroxynonenal, which have been shown to mediate inflammatory pain.[1]
|
| ln Vivo |
In the CFA-induced pain model, treatment with 100 mg/kg QD or 100 mg/kg BID ADX-102 resulted in statistically significant reductions in thermal hypersensitivity as measured by the Hargreave’s plantar test (Figure 1). Only the 100 mg/kg BID dose of ADX-102 showed an effect on mechanical sensitivity, as assessed by the Von Frey force test (Figure 2). Paw thickness, a measure of swelling, showed a modest effect at the 30 and 100 mg/kg BID doses (Figure 3).[1]
In the carrageenan-induced pain model, ADX-102 treatment resulted in statistically significant reductions in thermal hypersensitivity at ADX-102 doses of 30 mg/kg BID and 100 mg/kg BID (Figure 4), but did not affect mechanical hypersensitivity (Figure 5). Paw thickness, a measure of swelling, showed a modest effect at the 100 mg/kg QD dose (Figure 6). There were no changes in body weight as a result of treatment in any group.[1] |
| Animal Protocol |
The effect of ADX-102 on acute inflammatory pain was tested in the carrageenaninduced and Complete Freund’s Adjuvant (CFA)-induced models in mice [1].
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| References |
[1]. Susan Macdonald, et al. ADX-102, a novel aldehyde trap, reduces nociceptive behavior in mouse models of carrageenan and CFA induced pain.https://ir.aldeyra.com/static-files/527c5795-0792-4322-9f47-69c79879415a
[2]. Reproxalap Phase 2b Dry Eye Disease Results.https://ir.aldeyra.com/static-files/c642ef41-fe14-47d1-ba0e-d2b6a90f6a57 |
| Additional Infomation |
Reproxalap (previously ADX 102 or NS-2) is a small molecule inhibitor being developed by Aldeyra Therapeutics investigated against dry eye disease, allergic conjunctivitis, noninfectious anterior uveitis, and Sjögren-Larsson syndrome. NS-2 has orphan drug status due to it being investigated for treatment of Sjogren-Larsson syndrome.
Mechanism of Action Reproxalap inhibits Reactive Aldehyde Species (RASP) and is being investigated against dry eye disease, allergic conjunctivitis, noninfectious anterior uveitis, and Sjögren-Larsson syndrome. |
| Molecular Formula |
C12H13CLN2O
|
|---|---|
| Molecular Weight |
236.697421789169
|
| Exact Mass |
236.071
|
| Elemental Analysis |
C, 60.89; H, 5.54; Cl, 14.98; N, 11.84; O, 6.76
|
| CAS # |
916056-79-6
|
| PubChem CID |
16088030
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| Appearance |
Typically exists as Light yellow to yellow solid at room temperature
|
| LogP |
2.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
16
|
| Complexity |
259
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GUHFUVLKYSQIOQ-UHFFFAOYSA-N
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| InChi Code |
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
|
| Chemical Name |
2-(3-amino-6-chloroquinolin-2-yl)propan-2-ol
|
| Synonyms |
NS-2; NS2 NS 2; ADX-102; Reproxalap; 916056-79-6; 2-(3-amino-6-chloroquinolin-2-yl)propan-2-ol; ADX-102; Reproxalap [USAN]; NS-2; ALD-102; F0GIZ22IJH; ADX102; ADX 102,
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~422.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (10.56 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2248 mL | 21.1238 mL | 42.2476 mL | |
| 5 mM | 0.8450 mL | 4.2248 mL | 8.4495 mL | |
| 10 mM | 0.4225 mL | 2.1124 mL | 4.2248 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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