產品描述: | 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 |
靶點: |
pIC50: 8.0 (human P2X3), 8.0 (rat P2X3), 7.3 (human P2X2/3);P2XReceptor |
體內研究: |
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 |
參考文獻: |
1. Gever JR, et al. AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-1398. 2. Munoz A, et al. Modulation of bladder afferent signals in normal and spinal cord-injured rats by purinergic P2X3 and P2X2/3receptors. BJU Int. 2012 Oct;110(8 Pt B):E409-414. |
溶解性: |
Soluble in DMSO |
保存條件: |
2-8℃,避光 |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.499 ml |
12.493 ml |
24.987 ml |
5 mM |
0.5 ml |
2.499 ml |
4.997 ml |
10 mM |
0.25 ml |
1.249 ml |
2.499 ml |
50 mM |
0.05 ml |
0.25 ml |
0.5 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |