Acloproxalap
Based on 1 Customer Validation
Acloproxalap (ADX-629) is an orally active reactive aldehyde species (RASP) inhibitor. Acloproxalap binds covalently to free aldehydes, sequesters reactive aldehyde species, malondialdehyde, acetaldehyde and preformed malondialdehyde-acetaldehyde adducts, and reduces elevated RASP levels. Acloproxalap decreases the formation of aldehyde adducts, reduces liver and serum triglyceride levels, hepatic fat accumulation, circulating anti-malondialdehyde-acetaldehyde adduct antibody levels, and inhibits the release of IL-6 and MCP-1. Acloproxalap improves cell viability of liver slices exposed to ethanol. Acloproxalap blocks ethanol-induced damage in animal models of alcoholic liver disease. Acloproxalap is applicable to research related to alcoholic liver disease, alcoholic fatty liver disease, non-alcoholic steatohepatitis, chronic cough, rheumatoid arthritis, ulcerative colitis and mild atopic asthma.
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- Pureté: 99.92%
- CAS No.: 1824609-67-7
- Formule: C12H14N2O
- Masse moléculaire:202.25
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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IL-6 |
ADX-629 (0.1-100 μM; 24-72 h) reduces acetaldehyde levels in precision-cut liver slices from C57/BL6 mice exposed to 25 mM ethanol. Among the tested conditions, 0.1 μM (24 h) induces the greatest reduction within 24 hours, and the reduction effect of 1 μM (72 h) is statistically significant at the 72-hour time point[2].
ADX-629 (0.1-100 μM; 24-72 h) reduces ethanol-induced elevation of triglycerides in precision liver slices from C57/BL6 mice. Among the tested conditions, 0.1 μM (24 h) produces the greatest reduction within 24 hours, while 1 μM (24, 48, and 72 h) significantly decreases triglyceride levels to the level of the control group at all three time points[2].
ADX-629 increases the cell viability of precision liver slices from C57/BL6 mice exposed to 25 mM ethanol, and this effect is detected by measuring lactate dehydrogenase and adenosine triphosphate levels[2].
Acloproxalap (0-200 μM; 30-minute pre-treatment) potently reduces FIB-MAA-induced IL-6 and MCP-1 release in PMA (HY-18739)-differentiated human monocytic U-937 macrophages; it exerts significant inhibitory effects at a concentration of 1 μM, reduces cytokine release to background levels at concentrations ≥10 μM, and shows no cytotoxicity at all tested doses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PMA-differentiated U-937 human monocytic macrophages
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Concentration:0, 1, 10, 50, 100, 200 μM (30-minute pre-treatment)
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Incubation Time:30 min (pre-treatment); 24 h (FIB-MAA incubation)
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Result:Significantly reduced IL-6 and MCP-1 release at 1 μM.
Reduced cytokine levels to background (unmodified fibrinogen) levels at concentrations ≥10 μM.
Showed no toxic effects, with >99% cell viability confirmed via LDH assay.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/BL6 (10- to 12-week-old female, ≥20 g, chronic/binge alcoholic liver disease model)[1]
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Dosage:400 mg/kg
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Administration:p.o.; single dose
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Result:Increased serum acetaldehyde to 37.5 µM from 8.3 µM in ethanol-only mice.
Decreased liver acetaldehyde to 146.2 µM/mg from 284.3 µM/mg in ethanol-only mice.
Reduced serum triglyceride levels to 112.2 mg/dL from 166.2 mg/dL in ethanol-only mice.
Reduced liver triglyceride levels to 157.4 mg/dL/mg of protein from 299.0 mg/dL/mg of protein in ethanol-only mice.
Reduced Oil Red O staining integrated density significantly.
Reduced Bodipy staining integrated density significantly.
Reduced liver malondialdehyde-acetaldehyde (MAA) antigen levels to 3.2 from 5.5 in ethanol-only mice.
Reduced serum anti-MAA antibody levels to 74.3 relative units from 232.6 relative units in ethanol-only mice.
Reduced serum alanine aminotransferase (ALT) levels to 26.3 IU/L from 43.8 IU/L in ethanol-only mice.
Reduced liver interferon-γ (IFN-γ) levels to 3.0 pg/mL/mg from 6.6 pg/mL/mg in ethanol-only mice.
Reduced liver monocyte chemoattractant protein-1 (MCP-1) levels to 15.62 pg/mL/mg from 47.5 pg/mL/mg in ethanol-only mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1824609-67-7
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Appearance Solid
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Masse moléculaire 202.25
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Formule C12H14N2O
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Color Light yellow to yellow
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SMILES
OC(C)(C)C1=NC2=C(C=C1N)C=CC=C2
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Synonyms
ADX-629
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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 (494.44 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 (12.36 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 (12.36 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 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 (281 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]. Duryee MJ, Aripova N, Hunter CD, Ruskamp RJ, et al. A novel reactive aldehyde species inhibitor prevents the deleterious effects of ethanol in an animal model of alcoholic liver disease. Int Immunopharmacol. 2022 Dec;113(Pt A):109400. [Content Brief]
[3]. Guilleminault L, et al. Drugs Targeting Cough Receptors: New Therapeutic Options in Refractory or Unexplained Chronic Cough. Drugs. 2024 Jul;84(7):763-777. [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 | 4.9444 mL | 24.7219 mL | 49.4438 mL | 123.6094 mL |
| 5 mM | 0.9889 mL | 4.9444 mL | 9.8888 mL | 24.7219 mL | |
| 10 mM | 0.4944 mL | 2.4722 mL | 4.9444 mL | 12.3609 mL | |
| 15 mM | 0.3296 mL | 1.6481 mL | 3.2963 mL | 8.2406 mL | |
| 20 mM | 0.2472 mL | 1.2361 mL | 2.4722 mL | 6.1805 mL | |
| 25 mM | 0.1978 mL | 0.9889 mL | 1.9778 mL | 4.9444 mL | |
| 30 mM | 0.1648 mL | 0.8241 mL | 1.6481 mL | 4.1203 mL | |
| 40 mM | 0.1236 mL | 0.6180 mL | 1.2361 mL | 3.0902 mL | |
| 50 mM | 0.0989 mL | 0.4944 mL | 0.9889 mL | 2.4722 mL | |
| 60 mM | 0.0824 mL | 0.4120 mL | 0.8241 mL | 2.0602 mL | |
| 80 mM | 0.0618 mL | 0.3090 mL | 0.6180 mL | 1.5451 mL | |
| 100 mM | 0.0494 mL | 0.2472 mL | 0.4944 mL | 1.2361 mL |
Acloproxalap Related Classifications
Cat. No.: HY-147240
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- Acloproxalap
- 1824609-67-7
- ADX-629
- ADX629
- ADX 629
- Interleukin Related
- malondialdehyde-acetaldehyde adducts
- malondialdehyde
- alcoholic liver disease
- U-937 human monocytic macrophages
- reactive aldehyde species
- C57/BL6 mouse precision cut liver slices
- macrophages
- acetaldehyde
- liver slices
- non-alcoholic steatohepatitis
- Inhibitor
- inhibitor
- inhibit