NRA-0160 是一种选择性的 <b>dopamine D4 receptor</b> 拮抗剂,<b>K<sub>i</sub></b> 值为 0.48 nM;同时对 <b>dopamine D2 receptor</b>,<b>D3 receptor</b>,大鼠 <b>5-HT2A receptor</b> 和 <b>α1 adrenoceptor</b> 分别具有不同程度的亲和度,<b>K<sub>i</sub></b> 值分别为 >10000 nM,39 nM,180 nM 和 237 nM。<BR><a href="https://www.medchemexpress.cn/HC-067047.html">HC-067047</a>产品描述:HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 ± 6 nM, 133 ± 25 nM, and 17 ± 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM).
target: TRPV4
IC 50: 48 ± 6 nM (human), 133 ± 25 nM (rat) , and 17 ± 3 nM (mouse)
1) The reference for administration of HC-067047 is 10 mg/kg (i.P)
2) HC-067047 caused a significant reduction of the maximal micturition pressure in rats, which might be caused by an effect on TRPV4 in smooth muscle.
3) HC-067047 Reduces Pollakisuria and Increases Functional Bladder Capacity
4) HC-067047 exhibits high selectivity toward TRPV4: IC50 values were at least 100-fold higher for the closely related channels TRPV1, TRPV2, and TRPV3, and 10-fold higher for TRPM8 and hERG.
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已为全球多个知名企业、院校构建各种定制型化合物库。</span><br><br>产品链接:<a href="http://www.medchemexpress.cn/HC-067047.html">www.medchemexpress.cn/HC-067047.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"
src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg"
alt="">Purity:98%<BR>MWt:439.5207<BR>Formula:C24H23F2N3OS<BR>SMILES:O=C(C1=NC(C2=CC=C(F)C=C2)=C(CCN3CC/C(CC3)=C\C4=CC=CC(F)=C4)S1)N<BR>Pathway:GPCR/G Protein; Neuronal Signaling; <BR>Mechanisms:5-HT Receptor; Adrenergic Receptor; Dopamine Receptor; <BR>Research Area:Neurological Disease<BR>电话: 021-58955995<BR>网址: www.MedChemExpress.cn <BR>地址: 上海市浦东新区蔡伦路720号2号楼3层
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