2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. E-6837

E-6837 是一种具有选择性的口服活性 5-HT6 受体配体。E-6837 通过监测 cAMP 信号通路，在假定沉默的大鼠 5-HT6 受体上表现出部分激动活性，在组成型激活的人源 5-HT6 受体上表现出完全激动活性。E-6837 可诱导摄食减少、降低脂肪量与体重，并改善血糖控制。E-6837 可用于肥胖症的相关研究。

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E-6837

E-6837 Chemical Structure

CAS No. : 528859-61-2

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E-6837 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
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

E-6837 is a selective and orally active 5-HT6 receptor ligand. E-6837 demonstrates partial agonism at a presumably silent rat 5-HT6 receptor and full agonism at a constitutively active human 5-HT6 receptor by monitoring the cAMP signaling pathway. E-6837 induces hypophagia, reduces fat mass and body weight, and improves glycemic control. E-6837 can be used for the research of obesity[1].

IC50 & Target[1]

Human 5-HT6 Receptor

9.13 (pKi)

Rat 5-HT6 Receptor

8.37 (pIC50)

Rat 5-HT6 Receptor

9.19 (pEC50)

Human 5-HT6 Receptor

9.53 (pEC50)

体外研究
(In Vitro)

E-6837 可选择性高亲和力结合 HEK-293 细胞膜制备物中的重组人源 5-HT6 受体 (pKi = 9.13 ± 0.17)[1]。
E-6837 可作为强效部分激动剂 (Emax = 67 ± 4%, pEC50 = 9.19 ± 0.11) 和部分拮抗剂 (Imax = 41 ± 3%, pIC50 = 8.37 ± 0.09) 作用于稳定表达在 HEK-293F 细胞中的、推测为沉默型的大鼠 5-HT6 受体[1]。
E-6837 是一种效力较强的近乎完全激动剂 (Emax = 96 ± 4%, pEC50 = 9.53 ± 0.09)，作用于稳定表达在 HEK-293F 细胞中的组成型活性人源 5-HT6 受体[1]。

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

E-6837 相关抗体:
体内研究
(In Vivo)

E-6837 (5-30 mg/kg；口服；单次给药) 在 30 mg/kg 剂量下可诱导雄性 Sprague-Dawley 大鼠出现持续 6 小时的短暂摄食抑制，而 5 mg/kg 剂量对摄食无影响[1]。
E-6837 (60 mg/kg；口服；单剂量) 不会在雄性 Sprague-Dawley 大鼠中诱导条件性味觉厌恶或高岭土摄食，表明该剂量下无催吐或厌恶效应[1]。
E-6837 (30 mg/kg；口服；每日 2 次；连续 28 天) 可诱导饮食诱导肥胖的雌性 Wistar 大鼠出现最高 15.7%的体重下降[1]。

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

Animal Model: Sprague-Dawley rats (male, 190 g at study start)[1]
Dosage: 5 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Reduced food intake transiently, with onset of suppression ~2 hours into the nightly feeding session, lasting ~6 hours (30 mg/kg dose).
Had no effect on food intake (5 mg/kg dose).
Did not alter locomotor activity (both doses) both.
Animal Model: Sprague-Dawley rats (male, 6 weeks old, ~190 g at study start)[1]
Dosage: 60 mg/kg
Administration: p.o.; single dose
Result: Did not elicit conditioned taste aversion, with a saccharin preference ratio of 77.0 ± 10.7% (72-84 h) similar to vehicle (up to 60 mg/kg dose).
Had no effect on kaolin consumption at tested doses.
Animal Model: Wistar rats (female, 250-300 g at study start, diet-induced obese via 12-week high-calorie cafeteria diet)[1]
Dosage: 30 mg/kg
Administration: p.o.; twice daily; 28 days
Result: Induced a maximal body weight loss of -15.7% over 28-day treatment period, with sustained weight loss for 3 weeks.
Reduced fat mass by 31.7%, with no significant changes in water, protein, or ash content.
Reduced plasma leptin levels by 49.6% (from 166 ± 19 ng/mL to 83 ± 19 ng/mL).
Improved glycemic control, with a significant reduction in plasma glucose excursion during glucose tolerance test and a trend toward reduced plasma insulin levels.
Resulted in transient rebound hyperphagia after treatment withdrawal, but body weight remained -6.6% lower than vehicle controls on day 71, with no profound rebound weight gain.
Decreased cumulative food intake by 31.7% during treatment period, with preferential reduction in chocolate intake.
分子量

427.95

Formula

C22H22ClN3O2S
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

E-6837 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:

E-6837528859-61-2E6837E 68375-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorSprague-Dawley5-HT6 receptorobesityfat masshypophagiaHEK-293F cellscAMP signaling pathwaysglycemic controldiet-induced obese female Wistar ratsHEK-293 membrane preparationsInhibitorinhibitorinhibit

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