5-HT2B antagonist-1

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].

Product Specifications

CAS Number

[393129-91-4]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Endocrinology; Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/5-ht2b-antagonist-1.html

Purity

99.90

Solubility

DMSO : ≥ 33.33 mg/mL|H2O : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

BrC1=CC=C(NC2=NC(N)=NC(C)(C)N2)C=C1

Molecular Formula

C11H14BrN5

Molecular Weight

296.17

Precautions

H315, H319

References & Citations

[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