293754-55-9 Usage
Uses
Used in Cholesterol Regulation:
T0901317 is used as a selective agonist for liver X receptors (LXRα and LXRβ) to regulate cholesterol metabolism. By acting through LXR and its RXR heterodimerization partner, T0901317 induces the expression of the ABCA1 reverse cholesterol transporter, which increases the efflux of cholesterol from enterocytes and inhibits overall cholesterol absorption.
Used in Atherosclerosis Prevention:
T0901317 is used as a potent LXR agonist to inhibit the development of atherosclerosis in LDL receptor-deficient mice. Its ability to raise HDL cholesterol and triglyceride levels, along with its anti-inflammatory properties, contribute to its potential as a therapeutic agent for atherosclerosis prevention.
Used in Diabetes Management:
T0901317 is used as a selective LXR agonist to lower plasma glucose levels in diabetic rodents. Its potential to improve insulin sensitivity and glucose metabolism makes it a candidate for diabetes management and treatment.
Used in Drug Discovery and Research:
T0901317 is used as a research tool in drug discovery and development for various applications, including the study of LXR and FXR pathways, cholesterol regulation, atherosclerosis prevention, and diabetes management. Its highly selective and potent agonist properties make it a valuable compound for investigating the mechanisms and potential therapeutic applications of these receptors in various diseases and conditions.
Biological Activity
Potent, high affinity liver X receptor (LXR) agonist (EC 50 ~ 50 nM, Kd values are 7 and 22 nM for LXR- α and LRXR- β respectively). Upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism. Decreases amyloid- β production in primary neurons in vitro . Displays an EC 50 of ~ 5 μ M for activation of bile acid farnesoid X receptors (FXRs); 10-fold more potent than natural FXR ligand chenodeoxycholic acid.
Biochem/physiol Actions
Cell permeable: yes
references
[1]. schultz j r, tu h, luk a, et al. role of lxrs in control of lipogenesis[j]. genes & development, 2000, 14(22): 2831-2838.[2]. kumar n, solt l a, conkright j j, et al. the benzenesulfoamide t0901317 [n-(2, 2, 2-trifluoroethyl)-n-[4-[2, 2, 2-trifluoro-1-hydroxy-1-(trifluoromethyl) ethyl] phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-α/γ inverse agonist[j]. molecular pharmacology, 2010, 77(2): 228-236.[3]. houck k a, borchert k m, hepler c d, et al. t0901317 is a dual lxr/fxr agonist[j]. molecular genetics and metabolism, 2004, 83(1): 184-187.[4]. liu y, yan c, wang y, et al. liver x receptor agonist t0901317 inhibition of glucocorticoid receptor expression in hepatocytes may contribute to the amelioration of diabetic syndrome in db/db mice[j]. endocrinology, 2006, 147(11): 5061-5068.
Check Digit Verification of cas no
The CAS Registry Mumber 293754-55-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,9,3,7,5 and 4 respectively; the second part has 2 digits, 5 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 293754-55:
(8*2)+(7*9)+(6*3)+(5*7)+(4*5)+(3*4)+(2*5)+(1*5)=179
179 % 10 = 9
So 293754-55-9 is a valid CAS Registry Number.
InChI:InChI=1/C17H12F9NO3S/c18-14(19,20)10-27(31(29,30)13-4-2-1-3-5-13)12-8-6-11(7-9-12)15(28,16(21,22)23)17(24,25)26/h1-9,28H,10H2
