1. GPCR/G Protein Neuronal Signaling
  2. Neurokinin Receptor
  3. SDZ NKT 343

SDZ NKT 343 是一种选择性的、具有口服活性的 NK1 receptor 拮抗剂,对人 NK1 受体的 IC50 为 0.62 nM。SDZ NKT 343 具有良好的镇痛活性。

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SDZ NKT 343 Chemical Structure

SDZ NKT 343 Chemical Structure

CAS No. : 180046-99-5

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查看 Neurokinin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity[1][2].

IC50 & Target

hNK1

0.62 nM (IC50)

hNK2

0.52 μM (Ki)

hNK3

3.4 μM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
COS-7 IC50
82.4 μM
Compound: 5k
In vitro binding affinity towards Tachykinin receptor 1 by measuring its ability to displace [3H]SP (0.6 nM) binding to membranes from Cos-7 cells transiently transfected with the hNK-1R
In vitro binding affinity towards Tachykinin receptor 1 by measuring its ability to displace [3H]SP (0.6 nM) binding to membranes from Cos-7 cells transiently transfected with the hNK-1R
[PMID: 9703462]
体外研究
(In Vitro)

SDZ NKT 343 shows a markedly lower affinity at rat NK1 receptors in whole forebrain membranes (IC50=451+139 nM)[1].
SDZ NKT 343 shows weak affinity to human NK2 and NK3 receptors in transfected Cos-7 cells (Ki of 0.52+0.04 μM and 3.4+1.2 μM respectively)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SDZ NKT 343 antagonized [Sar9]SP sulphone-evoked bronchoconstriction (70% reduction at 0.4 mg/kg, i.v.) in anaesthetized guinea-pigs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

579.65

Formula

C33H33N5O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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× = ×
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产品名称:
SDZ NKT 343
目录号:
HY-108480
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