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CAS No.: 916056-79-6

Reproxalap Catalog No. CSN27226

Synonyms: ADX-102;NS-2

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 .

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生物活性

描述By covalently binding amino and thiol groups on receptors and kinases, reactive aldehyde species(RASP) potentiate upstream proinflammatory signaling cascades that involve NF-kB, inflammasomes, scavenger receptor A, and other mediators^[3].Reproxalap(ADX-102) is a novel small-molecule RASP inhibitor in development to treat Noninfectious anterior uveitis(NAU), allergic conjunctivitis, and dry eye disease(DED). Results from nonclinical studies indicate that reproxalap and related molecules have the potential to mitigate ocular inflammation related to NAU and other inflammatory eye conditions, such as postsurgical inflammation and diabetic retinopathy^[4]. Reproxalap has been shown to outcompete biological targets for MDA and HNE to inhibit both helper T cell 1 (Th1)- and Th2-mediated inflammation in a number of animal models.In DED, the activity of reproxalap is potentially 2-fold, the result of modulation of inflammation and prevention of RASP modification of tear lipids, suggesting that reproxalap may represent an important new therapeutic approach for the treatment of DED^[5].In the CFA-induced pain model, treatment with 100 mg/kg QD or 100 mg/kg BID ADX-102 resulted in statistically significant reductions in thermal hypersensitivity.Only the 100 mg/kg BID dose of ADX-102 showed an effect on mechanical sensitivity. Paw thickness showed a modest effect at the 30 and 100 mg/kg BID doses. In the carrageenan-induced pain model, ADX-102 treatment resulted in statistically significant reductions in thermal hypersensitivity at ADX-102 doses of 30 mg/kg BID and 100 mg/kg BID, but did not affect mechanical hypersensitivity. Paw thickness showed a modest effect at the 100 mg/kg QD dose.There were no changes in body weight as a result of treatment in any group.ADX-102 mediated dose-dependent reductions in nociceptive behavior in both models of acute pain^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.2248 mL
- 21.1240 mL
- 42.2480 mL
- 5 mM
- 0.8450 mL
- 4.2248 mL
- 8.4496 mL
- 10 mM
- 0.4225 mL
- 2.1124 mL
- 4.2248 mL

技术信息

CAS号	916056-79-6	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C12H13ClN2O	运输	蓝冰
分子量	236.70	别名	ADX-102;NS-2

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