2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT2A antagonist 2

5HT2A antagonist 2 是一种具有选择性的，口服有效的 5HT2A 拮抗剂，IC50 为 14 nM。5-HT2A antagonist 2 具有良好的化学、肝细胞和血浆稳定性，在细胞系 VERO，HFL-1，L929，NIH3T3 和 CHO-K1 中不具备明显的细胞毒性。

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5-HT2A antagonist 2 Chemical Structure

5-HT2A antagonist 2 Chemical Structure

CAS No. : 2641482-08-6

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5-HT2A antagonist 2 相关抗体

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查看 5-HT Receptor 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1[1].

IC50 & Target

5-HT2A Receptor

14 nM (IC50)

体内研究
(In Vivo)

5-HT2A antagonist 2 (5-10 mg/kg，口服，每天，共 12 周) 可以预防 c57BL6J 小鼠中 HFD 诱导的代谢功能障碍相关的脂肪肝病(MASLD)[1]。
5-HT2A antagonist 2 (5-10 mg/kg，口服，每天，共 12 周) 抑制 CDAHFD 喂养的 C57BL6/J 小鼠的肝纤维化和炎症[1]。
5-HT2A antagonist 2 在老鼠和狗体内的药代动力学特性[1]：

5-HT2A antagonist 2 在老鼠和狗体内的药代动力学分析[1]

species route Dose (mg/kg) T1/2 (h) AUC (μg·h/mL) CL (L/h/kg) V (L/kg) F (%)
rat iv 5 4.4 1.55 2.82 8.86 -
dog iv 5 8.6 16.79 0.42 4.36 -
dog po 5 1.02 19.11 - - 73

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

Animal Model: HFD-fed C57BL6/J mice[1]
Dosage: 5-10 mg/kg
Administration: p.o., daily for 12 weeks
Result: Reduced fat mass and weight of liver and inguinal white adipose tissue (iWAT), improved glucose tolerance.
Reduced steatosis, lobular inflammation, and hepatocyte ballooning in liver tissue.
Animal Model: choline-deficient, L-amino acid-defined high-fat diet (CDAHFD) fed C57BL6/J mice[1]
Dosage: 5-10 mg/kg
Administration: p.o., daily for 12 weeks
Result: Decreased mRNA expressions of ol1a1 and α-SMA, decreased collagen accumulation and expressions of α-SMA, TNF-α, and IL-1β .
分子量

517.06

Formula

C30H33ClN4O2
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-HT2A antagonist 2 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:

5-HT2A antagonist 22641482-08-65-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorMetabolic Dysfunction-Associated Steatotic Liver DiseaseMASLDMetabolic Dysfunction-Associated SteatohepatitisMASHInhibitorinhibitorinhibit

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