omarigliptin  (Simson Pharma)

Journal: The Journal of Clinical Investigation

Article Title: Glucagon-like peptide-1 receptor agonists, but not dipeptidyl peptidase-4 inhibitors, reduce alcohol intake

doi: 10.1172/JCI188314

Figure Lengend Snippet: ( A ) Linagliptin (2.5, 5, 10, and 20 mg/kg, s.c.), tested using a between-subjects design (see ), had no effect on binge-like alcohol drinking, measured on the first 4-hour session (Tuesday) of each week, in mice ( n = 16 males, 16 females). Drug (linagliptin) effect: F 1,28 = 1.90, P = 0.18; week effect: F 3,8 = 1.04, P = 0.38; sex effect: F 1,28 = 0.80, P = 0.38, drug × week interaction: F 3,84 =0.16, P = 0.93; drug × sex interaction: F 1,28 =0.05, P = 0.82; week × sex interaction: F 3,84 = 2.12, P = 0.10; drug × week × sex interaction: F 3,84 = 1.07, P = 0.37. ( B ) Linagliptin (20 mg/kg, i.p.), tested using a between-subjects design, lowered blood glucose levels following both glucose ( n = 8 males, 8 females) and glucose-plus-alcohol ( n = 8 males, 8 females) challenge tests in mice. Drug (linagliptin) effect: F 1,28 = 11.16, P = 0.002; alcohol effect: F 1,28 = 12.19, P = 0.002 (glucose alone > glucose plus alcohol); drug × alcohol interaction: F 1,28 = 0.52, P = 0.48. ( C ) Omarigliptin (10, 20 mg/kg, i.p.), tested using a within-subjects design (see ), had no effect on binge-like alcohol drinking in mice ( n = 4 males, 3 females). Drug (omarigliptin) effect: F 2,10 = 0.04, P = 0.96; sex effect: F 1, 5 = 0.51, P = 0.51; drug × sex interaction: F 2,10 = 0.52, P = 0.61. ( D ) Omarigliptin (20 mg/kg, i.p.), tested using a between-subjects design, lowered blood glucose levels following both glucose ( n = 8 males, 8 females) and glucose plus alcohol ( n = 8 males, 8 females) challenge tests in mice. Drug (omarigliptin) effect: F 1,28 = 13.99, P = 0.0008; alcohol effect: F 1,28 = 0.12, P = 0.73; drug × alcohol interaction: F 1,28 = 0.16, P = 0.69. Individual data symbols are shown in black for males and in gray for females. Data are expressed as mean (SEM). ** P < 0.01, *** P < 0.001.

Article Snippet: Linagliptin (Cayman Chemical) and omarigliptin (TargetMol) were prepared with 5% Tween 80 (v/v; Thermo Fisher Scientific) and 0.9% saline.

Techniques:

Journal: The Journal of Clinical Investigation

Article Title: Glucagon-like peptide-1 receptor agonists, but not dipeptidyl peptidase-4 inhibitors, reduce alcohol intake

doi: 10.1172/JCI188314

Figure Lengend Snippet: ( A ) Linagliptin (10, 20 mg/kg, i.p.), tested using a within-subjects design (see ), had no effect on operant oral alcohol self administration in alcohol-dependent rats ( n = 10 males, 9 females). Drug (linagliptin) effect: F 2,34 = 2.01, P = 0.15; sex effect: F 1,17 = 0.18, P = 0.68; drug × sex interaction: F 2,34 = 1.75, P = 0.19. ( B ) Omarigliptin (10, 20 mg/kg, i.p.), tested using a within-subjects design (see ), had no effect on operant oral alcohol self administration in alcohol-dependent rats ( n = 10 males, 9 females). Drug (omarigliptin) effect: F 2,34 = 1.73, P = 0.19; sex effect: F 1,17 = 6.99, P = 0.02 (female > male); drug × sex interaction: F 2,34 = 0.82, P = 0.45. Individual data symbols are shown in black for males and in gray for females. Data are expressed as mean (SEM).

Article Snippet: Linagliptin (Cayman Chemical) and omarigliptin (TargetMol) were prepared with 5% Tween 80 (v/v; Thermo Fisher Scientific) and 0.9% saline.

Techniques:

Journal: The Journal of Clinical Investigation

Article Title: Glucagon-like peptide-1 receptor agonists, but not dipeptidyl peptidase-4 inhibitors, reduce alcohol intake

doi: 10.1172/JCI188314

Figure Lengend Snippet: ( A ) Effect of linagliptin on drinking-in-the-dark in mice was tested using a between-subjects design. Mice were assigned to 1 of the 2 groups: vehicle or linagliptin. The vehicle group received vehicle once a week for 4 weeks, whereas the linagliptin group received escalating doses of linagliptin (2.5, 5, 10, and 20 mg/kg, s.c.), 1 injection per week (Tuesdays). Sweetened alcohol solution was given for 4 hours on Tuesdays (results in ) and Fridays (results in ) and for 2 hours on Mondays and Thursdays (data not shown). ( B ) Effect of omarigliptin on drinking-in-the-dark in mice was tested using a within-subjects design. Mice received vehicle and 2 doses of omarigliptin (10, 20 mg/kg, i.p.) in a randomized (Latin-square) order on each 4-hour drinking test day (Tuesday/Friday; results in ). Sweetened alcohol solution was given for 2 hours on Mondays and Thursdays (data not shown). ( C ) Effects of linagliptin and omarigliptin on operant oral self administration in alcohol-dependent rats were tested using a within-subjects design. Rats were first made dependent using alcohol vapor exposure. They received daily, intermittent cycles of 14 hours of alcohol vapor exposure and 10 hours off (withdrawal). Operant oral alcohol self administration was performed 6–8 hours into withdrawal. Male rats were tested first with linagliptin then omarigliptin (as shown in the figure). Female rats were tested first with omarigliptin then linagliptin (opposite of the order shown in the figure). Linagliptin and omarigliptin testing was separated by at least 4 days (washout). Rats received vehicle and 2 doses of linagliptin (10, 20 mg/kg, i.p.; results in ) or vehicle and 2 doses of omarigliptin (10, 20 mg/kg, i.p.; results in ) in a randomized (Latin-square) order on each test day (Tuesday and Friday). Alcohol intake was measured after each 30-minute, fixed ratio 1, operant self-administration session.

Article Snippet: Linagliptin (Cayman Chemical) and omarigliptin (TargetMol) were prepared with 5% Tween 80 (v/v; Thermo Fisher Scientific) and 0.9% saline.

Techniques: Injection

Journal: Cell reports

Article Title: Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer

doi: 10.1016/j.celrep.2023.113198

Figure Lengend Snippet: KEY RESOURCES TABLE

Article Snippet: Omarigliptin , Cayman Chemical , Cat# 1226781-44-7.

Techniques: Recombinant, Protease Inhibitor, Plasmid Preparation, SYBR Green Assay, ISH Cell Assay, Sequencing, Software