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化學性質(zhì):
規(guī)格 | 10mg 50mg |
CAS | 18200-13-0 |
別名 |
|
化學名 | N-(2-(2H-tetrazol-5-yl)phenyl)-5,6,7,8-tetrahydronaphthalen-1-amine |
分子式 | C17H17N5 |
分子量 | 291.35 |
溶解度 | <29.14mg/ml in 1eq. NaOH; <29.14mg/ml in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
[(5, 6, 7, 8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine], named BL 1249, is a putative potassium channel opener with bladder-relaxant properties. In cultured bladder smooth muscle cells, BL 1249 decreased DiBAC4 (3) fluorescence in a concentration-dependent manner with an EC50 of 1.26 ± 0.6 μM. In human bladder cells, BL 1249 resulted in hyperpolarization in a concentration-dependent manner and yielded an EC50 of 1.49±0.08 μM. BL 1249 relaxed 30 mM KCl precontracted bladder strips in a concentration-dependent manner and yielded an EC50 of 1.1 ± 0.37 μM [1].
There are several types of potassium channels in urinary bladder myocytes and they are important in determining contractility and excitability of bladder smooth muscle. These channels include maxi-K+, KATP, members of the voltage-gated Kv family, SK family and, possibly, members of the KCNQ family. Open potassium channels can increase potassium efflux from the cell and produce membrane potential hyperpolarization, thereby decrease the activation of voltage-dependent calcium channels [1].
In human bladder myocytes, BL 1249 produced large instantaneously non-inactivating, activating outward currents that were readily reversible following drug washout. The BL 1249-induced current was hence of a reversal potential of near -80 mV under the physiological K+ gradient, this indicated that the current is carried by K+ ions [1].
特別提醒:
1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區(qū)。
2. 為了您的安全和健康,請穿好實驗服并佩戴一次性手套和口罩操作。
原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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