- GSK 2837808A
- Gimeracil
- Mycophenolate Mofetil
- PluriSIn #1 (NSC 14613)
- AGI-5198
| BVT 273311beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.82%
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Chemical structure
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| Cas No. | 376640-41-4 | SDF | Download SDF |
| Chemical Name | 3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide | ||
| Canonical SMILES | CC1=C(Cl)C=CC=C1S(NC2=NC(CC(N3CCN(CC3)C)=O)=CS2)(=O)=O | ||
| Formula | C17H21ClN4O3S2 | M.Wt | 428.96 |
| Solubility | ≥42.9mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Ki: 1 μM using 11-dehydrocorticosterone as substrate
BVT 2733 is a novel, small molecule, non-steroidal, and selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
11β-HSD1 has been reported to alter glucocorticoid hormone action in target tissues for insulin action and is suggested to play a key role in glucose homeostasis.
In vitro: BVT 2733 was identified as a novel type 1 selective inhibitor of murine 11β-HSD1 (Ki 1 μmol/l), which did not inhibit mouse 11β-HSD type 2 at a concentration as high as 200 μmol/l (corresponding to a Ki >33 μmol/l). Therefore, the selectivity of BVT 2733 for the 11β-HSD type 1 enzyme over the type 2 enzyme was estimated to be at least 30-fold based on the Ki values [1].
In vivo: In mice, BVT 2733 treatment could lower hepatic PEPCK and glucose-6-phosphatase mRNA, serum insulin and blood glucose concentrations compared with vehicle treated mice. In contrast, hepatic 11beta-hydroxysteroid dehydrogenase type 1 mRNA, liver function marker enzyme expression including alanine aminotransferase, aspartate aminotransferase and alkaline phosphatases, body weight as well as daily food intake were not changed by the treatment of BVT 2733 [1].
Clinical trial: Up to now, BVT 2733 is still in the preclinical development stage.
Reference:[1] Alberts P,Engblom L,Edling N,Forsgren M,Klingstrm G,Larsson C,Rnquist-Nii Y,Ohman B,Abrahmsén L. Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice. Diabetologia.2002 Nov;45(11):1528-32.
