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Reproxalap

Cat. No. M30897
Reproxalap Structure
Synonym:

ADX-102; NS-2

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 130  USD130 In stock
25mg USD 260  USD260 In stock
50mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 236.7
Formula C12H13ClN2O
CAS Number 916056-79-6
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bill Cavanagh, et al. Ophthalmol Ther. Reproxalap Activity and Estimation of Clinically Relevant Thresholds for Ocular Itching and Redness in a Randomized Allergic Conjunctivitis Field Trial

[2] David Clark, et al. Clin Ophthalmol. Reproxalap Improves Signs and Symptoms of Allergic Conjunctivitis in an Allergen Chamber: A Real-World Model of Allergen Exposure

[3] David McMullin, et al. Clin Ophthalmol. A Post-Acute Ocular Tolerability Comparison of Topical Reproxalap 0.25% and Lifitegrast 5% in Patients with Dry Eye Disease

[4] David Clark, et al. Am J Ophthalmol. Clinically Relevant Activity of the Novel RASP Inhibitor Reproxalap in Allergic Conjunctivitis: The Phase 3 ALLEVIATE Trial

[5] Kenneth J Mandell, et al. J Ocul Pharmacol Ther. Randomized Phase 2 Trial of Reproxalap, a Novel Reactive Aldehyde Species Inhibitor, in Patients with Noninfectious Anterior Uveitis: Model for Corticosteroid Replacement

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Keywords: Reproxalap, ADX-102; NS-2 supplier, RASP, inhibitors, activators


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