1. GPCR/G Protein Neuronal Signaling
  2. GPR119
  3. K-833

K-833 是一种 GPR119 激动剂,其对人、小鼠、大鼠和狗的 EC50 值分别为 39.8 nM、100 nM、75.4 nM和 12.6 nM。K-833 在小鼠急性肠道肽分泌中可使胰高血糖素样肽-1 (GLP-1) 分泌适度增加,与 AM-5262 (HY-16619) 联用时可协同提高 GLP-1 水平。K-833 可用于减轻体重的研究。

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K-833

K-833 Chemical Structure

CAS No. : 2639936-77-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

K-833 is a GPR119 agonist with EC50 values of 39.8 nM (human), 100nM (mouse), 75.4 nM (rat) and 12.6 nM (dog). K-833 demonstrates a modest increase in GLP-1 secretion and leads to a synergistic increase in GLP-1 levels when combined with AM-5262 (HY-16619) in acute gut peptide secretion assays in mice. K-833 can be used in studies on weight loss[1].

体外研究
(In Vitro)

K-833 对人 M1 受体表现出适度的拮抗作用 (IC50 = 4.5 μM),并能抑制激动剂与人非选择性 sigma 受体的结合 (IC50 = 2.7 μM),同时对 CYP2B6 具有中度可逆抑制作用 (IC50 = 8.6 μM)[1]

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

体内研究
(In Vivo)

K-833 (30 mg/kg,灌胃,单剂量) 在小鼠急性肠道肽分泌中可使胰高血糖素样肽-1 (GLP-1) 的分泌适度增加[1]

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

Animal Model: Male 10-12 week old C57BL/6J mice[1]
Dosage: 30 mg/kg or combined with AM-5262 (HY-16619) (30 mg/kg)
Administration: i.g. for a single dose
Result: Led to a modest increase in GLP-1 secretion.
Led to a synergistic increase in GLP-1 levels when combined with AM-5262.
分子量

640.14

Formula

C30H43ClFN5O7

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
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  • 稀释计算器

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  • 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.

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产品名称:
K-833
目录号:
HY-175422
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