Reproxalap
Based on 1 Customer Validation
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.
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- Pureté: 98.49%
- CAS No.: 916056-79-6
- Formule: C12H13ClN2O
- Masse moléculaire:236.70
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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PKCα |
Caspase 3 |
Caspase-7 |
Reproxalap (1 μM-10 mM; 1-24 h) causes a significant decrease in the viability of BEAS-2B and 16HBE cells, and dose-dependently reverses the slowing of BEAS-2B cell migration induced by 5% cigarette smoke extract[1].
Reproxalap (100-300 μM; 24 h) protects FAA-K1A cells from the cytotoxicity of C18:0-al[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BEAS-2B, 16HBE
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Concentration:0.1 μM, 1 μM, 10 μM, 100 μM, 1 mM, 10 mM
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Incubation Time:24 h
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Result:Showed no significant change in cell viability at 0.1-10 μM (BEAS-2B).
Significantly decreased cell viability at 1-10 mM (BEAS-2B).
Showed no significant change in cell viability at 0.1-100 μM (16HBE).
Significantly decreased cell viability at 1-10 mM (16HBE).
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Carrageenaninduced and Complete Freund’s Adjuvant (CFA)-induced models in mice[3]
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Dosage:30, 100 mg/kg; once a day or twice a day
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Administration:
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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.
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Animal Model:A mouse knockout model (abcr-/-) of macular degeneration (MD) [5]
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Dosage:10 mg/kg; single dose
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced the formation of N-retinylidene-N-retinylethanolamine (A2E) in the retina by 71% without affecting dark adaptation or body weight.
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Animal Model:A rat model of lipopolysaccharide (LPS)-induced uveitis[5]
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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
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Administration:Intravitreal (IVT)
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Result:Improved the eye examination scores, enhancing the retinal-choroidal ratings.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 916056-79-6
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Appearance Solid
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Masse moléculaire 236.70
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Formule C12H13ClN2O
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Color Light yellow to yellow
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SMILES
CC(C1=NC2=C(C=C(Cl)C=C2)C=C1N)(O)C
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Synonyms
ADX-102; NS-2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (422.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (10.56 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[2]. Rizzo WB, et al. Sjögren-Larsson syndrome: A biochemical rationale for using aldehyde-reactive therapeutic agents. Mol Genet Metab Rep. 2021 Dec 23;30:100839. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.2248 mL | 21.1238 mL | 42.2476 mL | 105.6189 mL |
| 5 mM | 0.8450 mL | 4.2248 mL | 8.4495 mL | 21.1238 mL | |
| 10 mM | 0.4225 mL | 2.1124 mL | 4.2248 mL | 10.5619 mL | |
| 15 mM | 0.2817 mL | 1.4083 mL | 2.8165 mL | 7.0413 mL | |
| 20 mM | 0.2112 mL | 1.0562 mL | 2.1124 mL | 5.2809 mL | |
| 25 mM | 0.1690 mL | 0.8450 mL | 1.6899 mL | 4.2248 mL | |
| 30 mM | 0.1408 mL | 0.7041 mL | 1.4083 mL | 3.5206 mL | |
| 40 mM | 0.1056 mL | 0.5281 mL | 1.0562 mL | 2.6405 mL | |
| 50 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1124 mL | |
| 60 mM | 0.0704 mL | 0.3521 mL | 0.7041 mL | 1.7603 mL | |
| 80 mM | 0.0528 mL | 0.2640 mL | 0.5281 mL | 1.3202 mL | |
| 100 mM | 0.0422 mL | 0.2112 mL | 0.4225 mL | 1.0562 mL |
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