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Reproxalap  (Synonyms: ADX-102; NS-2)

Cat. No.: HY-107150 Purity: 98.85%
Data Sheet SDS COA Handling Instructions Technical Support

Reproxalap (ADX-102) is an active aldehyde sequestering agent that's being researched for dry eye syndrome, allergic conjunctivitis, and non-infectious anterior uveitis. Reproxalap has anti-inflammatory and pain-relieving effects.

For research use only. We do not sell to patients.

Reproxalap Chemical Structure

Reproxalap Chemical Structure

CAS No. : 916056-79-6

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10 mM * 1 mL in DMSO
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Description

Reproxalap (ADX-102) is an active aldehyde sequestering agent that's being researched for dry eye syndrome, allergic conjunctivitis, and non-infectious anterior uveitis. Reproxalap has anti-inflammatory and pain-relieving effects[1][2][3].

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[1].
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[3].
Reproxalap (25-50 μg, IVT, injected in five doses after LPS (HY-D1056) induction) can improve eye scores in uveitis rats[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Carrageenaninduced and Complete Freund’s Adjuvant (CFA)-induced models in mice[1]
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) [3]
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[3]
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.
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT03131154Aldeyra Therapeutics, Inc.
Non-infectious Anterior Uveitis
April 26, 2017Phase 3
NCT03012165Aldeyra Therapeutics, Inc.|ORA, Inc.
Conjunctivitis, Allergic
December 2016Phase 2
NCT04735393Aldeyra Therapeutics, Inc.
Dry Eye Disease
January 26, 2021Phase 3
Molecular Weight

236.70

Formula

C12H13ClN2O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1=NC2=C(C=C(Cl)C=C2)C=C1N)(O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.85%

References

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
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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Reproxalap
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