1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate manufacturers
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| | 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate Basic information |
| | 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate Chemical Properties |
| Melting point | 95 - 96°C | | Boiling point | 486.7±45.0 °C(Predicted) | | density | 1.296±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Chloroform (Slightly), Methanol (Slightly, Heated) | | pka | 3.87±0.50(Predicted) | | form | powder | | color | off-white to tan |
| | 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate Usage And Synthesis |
| Uses | GSK 4112 is a synthetic ligand for REV-ERBα, a member of the nuclear receptor superfamily that functions as a receptor for the porphoryin heme. GSK 4112 mimics the action of heme acting as agonist and suppresses the expression of REV-ERBα target genes involved in gluconeogenesis. | | Biochem/physiol Actions | GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba. | | in vivo | GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage[2]. | Animal Model: | Male C57BL/6 mice with Fas-induced acute hepatic damage[2] | | Dosage: | 25 mg/kg | | Administration: | Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure | | Result: | Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis. |
| | storage | Store at +4°C |
| | 1,1-Dimethylethyl-N-[(4-chlorophenyl)methyl]-N-[(5-nitro-2-thienyl)methyl])glycinate Preparation Products And Raw materials |
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