For research use only. Not for therapeutic Use.
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].
| Catalog Number | I043433 |
| CAS Number | 393129-91-4 |
| Synonyms | 2-N-(4-bromophenyl)-4,4-dimethyl-1H-1,3,5-triazine-2,6-diamine |
| Molecular Formula | C11H14BrN5 |
| Purity | ≥95% |
| InChI | InChI=1S/C11H14BrN5/c1-11(2)16-9(13)15-10(17-11)14-8-5-3-7(12)4-6-8/h3-6H,1-2H3,(H4,13,14,15,16,17) |
| InChIKey | NZEZISMBIMCMOR-UHFFFAOYSA-N |
| SMILES | CC1(N=C(NC(=N1)NC2=CC=C(C=C2)Br)N)C |
| Reference | [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 |
