2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. CGP 12177

CGP 12177  (Synonyms: (±)-CGP 12177)

目录号: HY-101393
产品使用指南 技术支持

CGP 12177 ((±)-CGP 12177) 是一种 β- 肾上腺素能受体 (β-AR) 配体。CGP 12177 是 β3-AR 激动剂 (Ki = 88 nM)，同时具有 β1/β2-AR 拮抗作用 (β1 的 Ki = 0.9 nM；β2 的 Ki = 4 nM)。CGP 12177 在大鼠肺动脉中对 α1-AR 表现出部分激动剂特性。CGP 12177 可调节 NMRI 小鼠脂肪组织中 ucp 和瘦素基因的表达。CGP 12177 可用于心血管及代谢疾病相关研究[1][2][3][4]。

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CGP 12177

CGP 12177 Chemical Structure

CAS No. : 81047-99-6

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CGP 12177 的其他形式现货产品:

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Other Forms of CGP 12177:

CGP 12177 相关抗体

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

IC50 & Target[1][4]

Beta-1 adrenergic receptor

0.9 nM (Ki)

Beta-2 adrenergic receptor

4 nM (Ki)

Beta-3 adrenergic receptor

88 nM (Ki)

α1-adrenergic receptor

 

体外研究
(In Vitro)

CGP 12177 (0.01-100 μM) 以浓度依赖的方式增强 3 μM Prostaglandin F2α (PGF2α) (HY-12956) 诱导的大鼠肺叶内动脉张力，同时在用 30 nM Phenylephrine (PHE) (HY-B0769) 预收缩的动脉中诱导浓度依赖性的舒张[1]。
CGP 12177 (0.01-100 μM) 在基础张力下对大鼠肺叶内动脉的影响很小，但在 PGF2α (3 μM) 存在下可引起收缩作用，并显著增强 PHE 诱导的收缩[1]。
CGP 12177 (1-100 μM) 在加载了 Fura pentakisester-3 (PE-3) 并用 PGF2α 预收缩的大鼠加压动脉中，诱导细胞内钙浓度增加[1]。
CGP 12177 (100 μM，15 分钟) 对大鼠肺叶内动脉的基础张力无显著影响，但可使 PHE 的浓度-反应曲线右移，且最大反应无变化[1]。
在经 PGF2α 预收缩的大鼠肺内动脉中，CGP 12177 (1-100 μM) 诱导的收缩可被 Phentolamine (1 μM)、Phenoxybenzamine (1 μM)、SR 59230A (3 μM) 和 Bupranolol (5 μM) 抑制[1]。
CGP 12177 可完全且浓度依赖性地置换 [3H] 哌唑嗪的特异性结合，其 pKi 值为 5.22[1]。
CGP 12177 (0-10 μM, 30 分钟) 在 CHO-K1 细胞中，不会刺激 GFP 标记的人 β2- 肾上腺素能受体的内化[2]。
CGP 12177 作为高亲和力的部分激动剂，在表达人 β2- 肾上腺素能受体的 CHO-K1 细胞中可诱导 cAMP 积累和 CRE 介导的基因转录[2]。

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

CGP 12177 相关抗体:
体内研究
(In Vivo)

CGP 12177 (0.05、0.2、0.5 和 1 mg/kg，皮下注射，每日一次，持续 15 天) 可同时在 NMRI 小鼠脂肪组织中刺激特定 ucp 基因及瘦素基因的表达[3]。

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

Animal Model: Male NMRI mice (4-weeks old)[3]
Dosage: 0.05, 0.2, 0.5 and 1mg/kg
Administration: s.c., daily for 15 days
Result: Significantly decreased expression of the mRNAs for UCP1, UCP2 and UCP3 in brown adipose tissue (BAT) at the lower doses compared to control.
Slightly increased expression of the mRNAs for UCP1, UCP2 and UCP3 in brown adipose tissue (BAT) at the higher doses compared to control.
Markedly enhanced UCP1 mRNA expression in both white adipose tissue (WAT) depots (inguinal IWAT and epididymal EWAT) in a dose-dependent manner, the increase was from low (and variable) basal levels in IWAT and from undetectable levels in EWAT of control animals.
Upregulated UCP3 mRNA expression in WAT especially in EWAT and, to a lesser extent, in IWAT.
Did not upregulated UCP2 mRNA expression in any WAT depot.
Showed a decreased expression of UCP2 mRNA at doses lower than 1mg/kg in both IWAT and EWAT.
Regulated leptin mRNA levels in a tissue-dependent manner.
Showed no effect on leptin mRNA levels in EWAT at any dose.
Showed a 3-fold increase of leptin mRNA levels in BAT at 0.5 and 1mg/kg.
Resulted in a maximum of 2-fold stimulation in IWAT at 0.5 mg/kg.
Did not have any apparent effect on food intake, body weight or the weight of the analysed fat depots at any dose tested.
分子量

279.33

Formula

C14H21N3O3
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

CGP 12177 相关分类

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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.

Keywords:

CGP 1217781047-99-6(±)-CGP 12177CGP12177CGP-12177Adrenergic ReceptorBeta Receptorβ-ARβ2-ARβ1-ARsβ3-ARPGF2αα1-ARrat pulmonary arteryNMRI miceadipose tissuesInhibitorinhibitorinhibit

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