1401564-00-8
Chemical Structure
KR-67607
- CAS No.: 1401564-00-8
- Formula:C24H29Cl2F3N4O4S
- Molecular Weight:597.48
InChIKey: DYPNORVQVVTGPG-RGDYZCBCSA-N
SMILES: NC(C12C[C@]3([H])[C@H]([C@](CC(C3)C2)([H])C1)NC(CN4S(=O)(N(C5=C(C=C(C=C5Cl)C(F)(F)F)Cl)CC(C4)C)=O)=O)=O
Biological Activity: KR-67607 is a selective 11β-HSD1 inhibitor, with an IC50 value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease[1][2][3].
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KR-67607 | KR-67607 is a selective 11β-HSD1 inhibitor, with an IC50 value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease. | |||||||||||||||||||||
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- [1]. Choi KJ, et al. Protective effect of a novel selective 11β-HSD1 inhibitor on eye ischemia-reperfusion induced glaucoma. Biochem Pharmacol. 2019;169:113632. [Content Brief]
- [2]. Kim J Y, et al. The Effects of KR-67607 on Intraocular Pressure and Glaucomatous Optic Neuropathy[J]. Investigative Ophthalmology & Visual Science, 2019, 60(9): 643-643.
- [3]. Na YJ, et al. A Novel Selective 11β-HSD1 Inhibitor, (E)-4-(2-(6-(2,6-Dichloro-4-(Trifluoromethyl)Phenyl)-4-Methyl-1,1-Dioxido-1,2,6-Thiadiazinan-2-yl)Acetamido)Adamantan-1-Carboxamide (KR-67607), Prevents BAC-Induced Dry Eye Syndrome. Int J Mol Sci. 2020;21(10):3729. [Content Brief]
Keywords
