Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H28N2O8S2 |
| Molecular Weight | 500.586 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(OC)C=C(C=C1)S(=O)(=O)N2CCCN(CC2)S(=O)(=O)C3=CC(OC)=C(OC)C=C3
InChI
InChIKey=GJUFPAZNBPFNRI-UHFFFAOYSA-N
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
| Molecular Formula | C21H28N2O8S2 |
| Molecular Weight | 500.586 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:36:41 GMT 2023
by
admin
on
Sat Dec 16 11:36:41 GMT 2023
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| Record UNII |
F3EST236LD
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| Record Status |
Validated (UNII)
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| Record Version |
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F3EST236LD
Created by
admin on Sat Dec 16 11:36:41 GMT 2023 , Edited by admin on Sat Dec 16 11:36:41 GMT 2023
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DTXSID201025986
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admin on Sat Dec 16 11:36:41 GMT 2023 , Edited by admin on Sat Dec 16 11:36:41 GMT 2023
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1520267
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admin on Sat Dec 16 11:36:41 GMT 2023 , Edited by admin on Sat Dec 16 11:36:41 GMT 2023
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447410-57-3
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admin on Sat Dec 16 11:36:41 GMT 2023 , Edited by admin on Sat Dec 16 11:36:41 GMT 2023
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SB-756050
Created by
admin on Sat Dec 16 11:36:41 GMT 2023 , Edited by admin on Sat Dec 16 11:36:41 GMT 2023
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PRIMARY | A Single-blinded Randomized, Placebo-controlled, Staggered-parallel, Escalating-dose Study to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Oral SB756050 Administered for 6 Days to Subjects With Type 2 Diabetes Mellitus Purpose: This is an escalating dose study in subjects with T2DM, which will consist of four overlapping cohorts receiving 6 days of SB756050 to assess safety, pharmacokinetics, and pharmacodynamics. |
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ACTIVE MOIETY |
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, SB756050, in patients with T2D. Fiftyone subjects were randomized to receive either placebo or one of four doses of SB756050 for 6 days. A single 100mg dose of sitagliptin was coadministered on Day 6 to all subjects. SB756050 was well tolerated it was readily absorbed, exhibited nonlinear pharmacokinetics with a less than doseproportional increase in plasma exposure above 100 mg, and demonstrated no significant changes in exposure when coadministered with sitagliptin. SB756050 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.
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ACTIVE MOIETY |
Originator: GlaxoSmithKline; Class: Antihyperglycaemic; Mechanism of Action: GPBAR1 protein agonist; Highest Development Phase: Discontinued for Type 2 diabetes mellitus; Most Recent Event: 28 Feb 2009 Phase-II clinical trials in Type-2 diabetes mellitus in USA (PO)
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