Reproxalap (Synonyms: ADX-102; NS-2)

Name: Reproxalap
Brand: MedChemExpress
SKU: HY-107150
Rating: 4.5 (1 reviews)

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

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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

CAS No. : 916056-79-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 125	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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

Molecular Weight

236.70

Formula

C₁₂H₁₃ClN₂O

CAS No.

916056-79-6

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
10 mM	0.4225 mL	2.1124 mL	4.2248 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.85%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (248 KB) HNMR (130 KB) RP-HPLC (168 KB)

Handling Instructions (2659 KB)

References

[1]. Susan Macdonald, et al. ADX-102, a novel aldehyde trap, reduces nociceptive behavior in mouse models of carrageenan and CFA induced pain.

[2]. Reproxalap Phase 2b Dry Eye Disease Results.

[3]. Susan G. Macdonald, Ph.D., et al. Novel Small Molecule Aldehyde Sequestering Agents Demonstrate Broad Therapeutic Potential for Ocular Inflammation.

Complete Stock Solution Preparation Table

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

Reproxalap Related Classifications

Neurological Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Reproxalap916056-79-6ADX-102 NS-2ADX102ADX 102NS2NS 2NS-2OthersDry eye syndromeAllergic conjunctivitisStaphylococcal infectionAnti-inflammatoryPain reliefInhibitorinhibitorinhibit

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Reproxalap (Synonyms: ADX-102; NS-2)

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Complete Stock Solution Preparation Table

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