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编 号:F486602
分子式:C14H17IN4O2
分子量:400.21
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.

体内研究:
AF-353 (Ro-4) does not compromise oxygen levels or cardiac function.AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats.AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced.Animal Model:Female Sprague-Dawley rats (250–300 g) bearing SCI
Dosage:10 mg/kg, 20 mg/kg
Administration:Intravenous injection; interval of 90 minutes, for 4 hours to 6 hours
Result:Significantly reduced purinergic response in both normal and SCI rats.

体外研究:
AF-353 (Ro-4) is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels.AF-353 (Ro-4) also blocks human P2X2/3 channel function with marginally reduced potency with a p50 of 7.3.
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