5-HT2B antagonist-1 是一种具有口服活性的 5-HT2B 受体拮抗剂，其 IC50 值为 33.4 nM。可用于以 5-HT2B 受体信号传导为特征的疾病研究，如肝细胞癌、心血管疾病或胃肠道疾病。
货号:ajcx39834
CAS:393129-91-4
分子式:C11H14BrN5
分子量：296.17
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease[1][2].

5-HT2B antagonist-1 (compound 5g) has some sodium channel binding activity with IC50 values in the range of 12.6 to 57.5 μM[1].
5-HT2B antagonist-1 (coumpound 1-e) inhibits 5-HT2B receptor activity by less than 50% at 1 μM in CHO-K1 cell lines[3].

5-HT2B antagonist-1 (compound 15) (oral gavage, 30 mg/kg) can reduce visceral hypersensitivity significantly in irritable bowel syndrome (IBS) rats[2].

[1]. Xiang Ma, et al. Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5644
[2]. Yu Zhou, et al. Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. J Med Chem. 2016 Jan 28;59(2):707-20.
[3]. Huang Niu, et al. 5-HT2B Antagonists. WO2015158214

Protocol:

5-HT2BReceptor 33.4nM(IC50)