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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAdenosine amine congenerCat. No.: HY-128064CAS No.: 96760-69-9Synonyms: ADAC分式: CHNO分量: 576.6作靶點: Adenosine Receptor作通路: GPCR/G Protein儲存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實驗 DMSO : 31.

2、25 mg/mL (54.20 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.7343 mL 8.6715 mL 17.3430 mL5 mM 0.3469 mL 1.7343 mL 3.4686 mL10 mM 0.1734 mL 0.8672 mL 1.7343 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?,配制前請先配制澄的儲備液,再依次添加助溶?為保證實驗結(jié)果的可靠性,體內(nèi)實驗的作液,建

3、議您現(xiàn)現(xiàn)配,當天使;澄的儲備液可以根據(jù)儲存條件,適當保存;以下溶劑前的百分指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.61 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.61 mM); Clear solution3. 請依序添加每種溶劑: 10% DMSO 90% corn oilSolubilit

4、y: 2.08 mg/mL (3.61 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Adenosine amine congener (ADAC)種選擇性的 A1 腺苷受體 (A1 adenosine receptor) 激動劑,可以改善噪和鉑引起的蝸損傷。Adenosine amine congener 還具有神經(jīng)保護作。IC50 & Target A1 adenosine receptor 1 2體外研究 Adenosine amine congener

5、 can reduce oxidative stress in the noise-exposed cochlea, leading to protectionof sensory hair cells. Adenosine amine congener also can reduce cisplatin-induced apoptosis in cochleartissues, particularly in sensory hair cells and strial marginal cells. The mechanisms of otoprotection byAdenosine am

6、ine congener include inhibition of glutamate release via presynaptic A1 receptors and inhibitionof voltage-gated Ca2+ channels, which can prevent activation of apoptotic and necrotic cell death pathways1.體內(nèi)研究 Adenosine amine congener (25-300g/kg/day; intraperitoneal injection; daily; for 5 days; mal

7、e Wistar rats)treatment is most effective in the first 24 hours after noise exposure at doses 50g/kg, providing up to 21dB protection. Adenosine amine congener mitigates noise-induced hearing loss in a dose- and time-dependent manner 1.Animal Model: Male Wistar rats (8-10 weeks old) treated with noi

8、se exposure 1Dosage: 25 g/kg/day, 50 g/kg/day, 100 g/kg/day, 200 g/kg/day, and 300g/kg/dayAdministration: Intraperitoneal injection; daily; for 5 daysResult: Most effective in the first 24 hours after noise exposure at doses 50g/kg, and providedup to 21dB protection (averaged across 8-28kHz).REFEREN

9、CES1. Vlajkovic SM, et al. Adenosine amine congener as a cochlear rescue agent. Biomed Res Int. 2014;2014:841489.2. Vlajkovic SM, et al. Adenosine amine congener mitigates noise-induced cochlear injury. Purinergic Signal. 2010 Jun;6(2):273-81.McePdfHeightCaution: Product has not been fully validated for medical

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