2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT2C agonist-13

5-HT2C agonist-13 是一种口服有效的、选择性强且能穿透血脑屏障的 5-HT2C 受体激动剂，其对人 5-HT2C 受体的 EC50 为16 nM，Ki 为20 nM。5-HT2C agonist-13 能有效激活 5-HT2C 受体，减少食物摄入，降低体重增加，且其作用可被选择性 5-HT2C 拮抗剂逆转。5-HT2C agonist-13 可用于肥胖症的研究。

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5-HT2C agonist-13

5-HT2C agonist-13 Chemical Structure

CAS No. : 850033-84-0

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5-HT2C agonist-13 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-HT2C agonist-13 is an orally active, selective and brain-penetrant 5-HT2C receptor agonist with human 5-HT2C receptor EC50 of 16 nM, Ki of 20 nM. 5-HT2C agonist-13 functionally activates 5-HT2C receptors, reduces food intake, reduces body weight gain, and exhibits effects reversible by a selective 5-HT2C antagonist. 5-HT2C agonist-13 can be used for the research of obesity[1].

IC50 & Target[1]

Human 5-HT2C Receptor

16 nM (EC50)

Human 5-HT2C Receptor

20 nM (Ki)

5-HT2A Receptor

4926 nM (EC50)

5-HT2A Receptor

153 nM (Ki)

5-HT2B Receptor

1170 nM (EC50)

5-HT2B Receptor

431 nM (Ki)

体外研究
(In Vitro)

5-HT2C agonist-13 (compound 58) (10 pM-10 μM；45 分钟) 可与 HEK293E 细胞膜上表达的人重组 5-HT2C 受体强效结合，其 Ki 值为 20 nM，且相较于人 5-HT2B 和 5-HT2A 受体表现出结合选择性[1]。
5-HT2C agonist-13 (90 s-18 h) 可强效激活 HEK293E 细胞中表达的人源重组 5-HT2C 受体，其 EC50 为 16 nM；同时该化合物对人 5-HT2B 和 5-HT2A 受体具有高度功能选择性，对后两种受体仅发挥部分激动剂作用[1]。

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

5-HT2C agonist-13 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL Vss Tmax Cmax T1/2 AUC F
Rat[1] 4.4 mg/kg i.v. 37.4 mL/min/kg 4.8 L/kg / / / / /
Rat[1] 8.8 mg/kg p.o. / / 0.7 h 4050 nM 1.6 h 11000 nM·h 77 %
体内研究
(In Vivo)

5-HT2C agonist-13 (compound 58) (3-30 mg/kg；口服；单次给药) 可使雄性 Sprague Dawley 大鼠的进食量呈剂量依赖性降低，在 10 mg/kg 和 30 mg/kg 剂量下分别显著降低 32%和 41%[1]。
5-HT2C agonist-13 (10 mg/kg；口服；单次给药；与 SB-243213 联合给药) 在雄性 Sprague Dawley 大鼠中的摄食抑制作用可被选择性 5-HT2C 拮抗剂的联合给药完全逆转，证实该作用由 5-HT2C 受体介导[1]。
5-HT2C agonist-13 (3-30 mg/kg；口服；每日一次；连续 4 天) 可呈剂量依赖性降低瘦型 Sprague Dawley 大鼠的体重增长，在第 4 天 30 mg/kg 剂量下体重增长显著降低 6%[1]。
5-HT2C agonist-13 (300 mg/kg；口服；单次给药) 给药 24 小时后，不会在小鼠中引发胃壁细胞坏死或胃部损伤[1]。

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

Animal Model: Sprague Dawley (male, 250 g)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Caused a 12% reduction in food pellet consumption compared to vehicle.
Caused a statistically significant 32% reduction in food pellet consumption compared to vehicle.
Caused a statistically significant 41% reduction in food pellet consumption compared to vehicle.
Left water consumption and locomotor activity within normal ranges, and no overt physical or behavioral abnormalities were observed.
Animal Model: Sprague Dawley (male, 250 g)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose; co-administered with SB-243213
Result: Caused a 30% reduction in food intake that was completely reversed in a dose-dependent manner by co-administration of SB-243213.
Animal Model: Sprague Dawley (lean)[1]
Dosage: 3 mg/kg; 30 mg/kg
Administration: p.o.; daily; 4 days
Result: Caused a 1.6% reduction in body weight gain compared to vehicle on day 4.
Caused a statistically significant reduction in body weight gain as early as day 2, with a 6% reduction compared to vehicle on day 4.
Animal Model: Mice[1]
Dosage: 300 mg/kg
Administration: p.o.; single dose
Result: Did not cause gastric parietal cell necrosis or stomach lesions after 24 hours.
分子量

284.28

Formula

C14H15F3N2O
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

5-HT2C agonist-13 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

5-HT2C agonist-13850033-84-05-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2C receptorobesityHEK293E cellsHEK293E cell membranesbody weight gainSB-243213Sprague Dawley rats5-HT2B receptorfood intake5-HT2A receptorInhibitorinhibitorinhibit

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