For research use only. Not for therapeutic Use.
SB-756050（Cat No.:I009365）is a selective antagonist of the orexin-1 receptor (OX1R), a receptor involved in regulating arousal, wakefulness, and appetite. By inhibiting OX1R, SB-756050 has been investigated for its potential therapeutic use in treating conditions such as anxiety, sleep disorders, and addiction. Its ability to modulate orexin signaling makes it a valuable tool in studying the role of the orexin system in various physiological processes. Additionally, SB-756050 is used in research exploring novel treatments for conditions related to dysregulation of arousal and stress responses.
| Catalog Number | I009365 |
| CAS Number | 447410-57-3 |
| Synonyms | SB-756050; SB 756050; SB756050;1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane |
| Molecular Formula | C21H28N2O8S2 |
| Purity | ≥95% |
| Target | G protein-coupled Bile Acid Receptor 1 |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]-1,4-diazepane |
| InChI | InChI=1S/C21H28N2O8S2/c1-28-18-8-6-16(14-20(18)30-3)32(24,25)22-10-5-11-23(13-12-22)33(26,27)17-7-9-19(29-2)21(15-17)31-4/h6-9,14-15H,5,10-13H2,1-4H3 |
| InChIKey | GJUFPAZNBPFNRI-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C(C=C1)S(=O)(=O)N2CCCN(CC2)S(=O)(=O)C3=CC(=C(C=C3)OC)OC)OC |
| Reference | 1:Clin Pharmacol Drug Dev. 2013 Jul;2(3):213-22. doi: 10.1002/cpdd.34. Epub 2013 May 14. Safety, Pharmacokinetics, and Pharmacodynamic Effects of a Selective TGR5 Agonist, SB-756050, in Type 2 Diabetes.Hodge RJ,Lin J,Vasist Johnson LS,Gould EP,Bowers GD,Nunez DJ,SB-756050 Project Team, PMID: 27121782 DOI: 10.1002/cpdd.34 </br><span>Abstract:</span> TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D). We report here the safety, pharmacokinetics, and pharmacodynamic effects of a selective TGR5 agonist, SB-756050, in patients with T2D. Fifty-one subjects were randomized to receive either placebo or one of four doses of SB-756050 for 6 days. A single 100 mg dose of sitagliptin was co-administered on Day 6 to all subjects. SB-756050 was well-tolerated; it was readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose-proportional increase in plasma exposure above 100 mg, and demonstrated no significant changes in exposure when co-administered with sitagliptin. SB-756050 demonstrated highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB-756050 + sitagliptin were comparable to those of sitagliptin alone, even though gut hormone plasma profiles were different. This study was registered at ClinicalTrials.gov (NCT00733577). © The Author(s) 2013. |
