2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. NK3R antagonist-1

NK3R antagonist-1 是一种口服有效且可透过血脑屏障的神经激肽-3 受体 (NK3R) 拮抗剂，其在 CHO-K1 和 HEK293T 细胞中的 IC50 分别为 53.61 和 65.42 nM。NK3R antagonist-1 可降低去卵巢大鼠模型中的血浆黄体生成素 (LH) 水平。NK3R antagonist-1 可用于更年期潮热的相关研究。

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NK3R antagonist-1

NK3R antagonist-1 Chemical Structure

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NK3R antagonist-1 相关抗体

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NK1R NK2R NK3R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NK3R antagonist-1 is an orally active, blood-brain barrier permeable neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes[1].

IC50 & Target[1]

NK3R

53.61 nM (IC50)

体外研究
(In Vitro)

NK3R antagonist-1 (Compound 23i(R)) (0.30-30 μM) 可抑制 CHO-K1 细胞中的 hERG 钾通道，其 IC50 为 34.5 μM[1]。

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

NK3R antagonist-1 相关抗体:
体内研究
(In Vivo)

NK3R antagonist-1 (Compound 23i(R)) (120 mg/kg; i.g.; 单次给药) 可显著去势大鼠的血浆促黄体生成素水平，给药后最早 45 min 即可检测到其抑制活性[1]。

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

Animal Model: Sprague-Dawley (male, 8-12 weeks old, ovariectomized)[1]
Dosage: 120 mg/kg
Administration: i.g.; single dose
Result: Significantly reduced plasma luteinizing hormone (LH) levels, with inhibitory effect evident at 45 min post-dose, and statistically significant differences relative to vehicle control observed at both 45 and 90 min post-dose.
分子量

395.45

Formula

C20H18FN5OS
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

NK3R antagonist-1 相关分类

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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:

NK3R antagonist-1Neurokinin ReceptorNK receptorTachykinin receptorhuman NK3RHEK293T cellsCHO-K1 cell membrane preparationsovariectomized rat modelsmenopausal hot flashesblood-brain barrierluteinizing hormonehERG potassium channelsCHO-K1 cellsneurokinin-3 receptorInhibitorinhibitorinhibit

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NK3R antagonist-1
目录号：
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