2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. Neurokinin Receptor Endogenous Metabolite Calcium Channel
  4. WIN-64821

WIN-64821 是一种曲霉菌产生的次级代谢产物，一种神经激肽受体 (Neurokinin Receptor) 拮抗剂。WIN-64821 对 NK1、NK2、NK3 受体的 Ki 值分别为 0.24 (人星形细胞瘤细胞)、0.26 (大鼠十二指肠) 和 15.2 (豚鼠前脑) μM。WIN-64821 可抑制海兔肽诱导的大鼠输精管收缩，阻断 P 物质诱导的豚鼠回肠收缩和人星形细胞瘤细胞 Ca2+外流。WIN-64821 可用于镇痛和抗炎研究。

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WIN-64821

WIN-64821 Chemical Structure

CAS No. : 150881-27-9

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WIN-64821 相关抗体

Top Publications Citing Use of Products

查看 Neurokinin Receptor 亚型特异性产品:

查看所有亚型
NK1R NK2R NK3R

查看 Calcium Channel 亚型特异性产品:

查看所有亚型
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The Ki values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca2+ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research[1][2].

IC50 & Target[1]

NK1R

0.24 μM (Ki)

NK2R

0.26 μM (Ki)

NK3R

15.2 μM (Ki)

体外研究
(In Vitro)

WIN 64821 (1-10 μM; 10 minutes) 可作为豚鼠回肠条中 P 物质 (SP) 诱导收缩的竞争性功能拮抗剂，其 pA2 值为 6.6，对应的 EC50 为 0.63 μM[1]。
WIN 64821 (0.01-10 μM) 可抑制 P 物质诱导的人星形细胞瘤 U-373 MG 细胞 45Ca2+外流，平均 IC50 为 0.6 μM；且在 0.5、10 μM 浓度下本身不会诱导 45Ca2+外流[1]。
WIN 64821 可抑制大鼠输精管 (一种 NK2 功能模型) 中 NK2 功能模型诱导的抽搐增强作用，其平均 IC50 为 3.4 μM，且在最高 30 μM 的浓度下对基础抽搐高度无影响[1]。
WIN-64821 是人星形细胞瘤细胞上人 NK1 受体的竞争性拮抗剂，其 Ki 值为 230 nM[2]。
WIN-64821 是正常人胎儿组织中人类 NK1 受体的竞争性拮抗剂，其 Ki 值为 0.74 μM[2]。
WIN-64821 是豚鼠下颌下腺膜制备物中 NK1 受体的竞争性拮抗剂，其 Ki 值为 0.6 μM[2]。

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

WIN-64821 相关抗体:
分子量

664.77

Formula

C40H36N6O4
CAS 号
结构分类
初始来源

Aspergillus Species
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

WIN-64821 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WIN-64821150881-27-9WIN64821WIN 64821Neurokinin ReceptorEndogenous MetaboliteCalcium ChannelNK receptorTachykinin receptorCa2+ channelsCa channelsguinea pig NK1guinea pig ileumhuman NK2Aspergillus sp.rat NK2neurokinin receptorrat NK1NK3 neurokinin receptorshuman astrocytoma U-373 MG cellshuman NK1Inhibitorinhibitorinhibit

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