Adomeglivant - CAS 1488363-78-5
Catalog number: 1488363-78-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C32H36F3NO4
Molecular Weight:
555.64
COA:
Inquire
Targets:
Glucagon Receptor
Description:
Adomeglivant has been found to be a glucagon receptor antagonist that could probably be effective for both type-I and type-II diabetes mellitus.
Purity:
98%
Appearance:
Powder
Synonyms:
Adomeglivant; LY-2409021; Adomeglivant [USAN]; UNII-74Z5ZL2KVG; LY2409021; LY 2409021; 3-[[4-[(1S)-1-[4-(4-tert-butylphenyl)-3,5-dimethylphenoxy]-4,4,4-trifluorobutyl]benzoyl]amino]propanoic acid
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
Inquire
Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
FASLTMSUPQDLIB-MHZLTWQESA-N
InChI:
InChI=1S/C32H36F3NO4/c1-20-18-26(19-21(2)29(20)23-10-12-25(13-11-23)31(3,4)5)40-27(14-16-32(33,34)35)22-6-8-24(9-7-22)30(39)36-17-15-28(37)38/h6-13,18-19,27H,14-17H2,1-5H3,(H,36,39)(H,37,38)/t27-/m0/s1
Canonical SMILES:
CC1=CC(=CC(=C1C2=CC=C(C=C2)C(C)(C)C)C)OC(CCC(F)(F)F)C3=CC=C(C=C3)C(=O)NCCC(=O)O
Current Developer:
Eli Lilly
1.Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies.
Kazda CM;Ding Y;Kelly RP;Garhyan P;Shi C;Lim CN;Fu H;Watson DE;Lewin AJ;Landschulz WH;Deeg MA;Moller DE;Hardy TA Diabetes Care. 2016 Jul;39(7):1241-9. doi: 10.2337/dc15-1643. Epub 2015 Dec 17.
OBJECTIVE: ;Type 2 diabetes pathophysiology is characterized by dysregulated glucagon secretion. LY2409021, a potent, selective small-molecule glucagon receptor antagonist that lowers glucose was evaluated for efficacy and safety in patients with type 2 diabetes.;RESEARCH DESIGN AND METHODS: ;The efficacy (HbA1c and glucose) and safety (serum aminotransferase) of once-daily oral administration of LY2409021 was assessed in two double-blind studies. Phase 2a study patients were randomized to 10, 30, or 60 mg of LY2409021 or placebo for 12 weeks. Phase 2b study patients were randomized to 2.5, 10, or 20 mg LY2409021 or placebo for 24 weeks.;RESULTS: ;LY2409021 produced reductions in HbA1c that were significantly different from placebo over both 12 and 24 weeks. After 12 weeks, least squares (LS) mean change from baseline in HbA1c was -0.83% (10 mg), -0.65% (30 mg), and -0.66% (60 mg) (all P < 0.05) vs. placebo, 0.11%. After 24 weeks, LS mean change from baseline in HbA1c was -0.45% (2.5 mg), -0.78% (10 mg, P < 0.05), -0.92% (20 mg, P < 0.05), and -0.15% with placebo. Increases in serum aminotransferase, fasting glucagon, and total fasting glucagon-like peptide-1 (GLP-1) were observed; levels returned to baseline after drug washout.
2.Efficient Synthesis of β-CF3/SCF3-Substituted Carbonyls via Copper-Catalyzed Electrophilic Ring-Opening Cross-Coupling of Cyclopropanols.
Li Y;Ye Z;Bellman TM;Chi T;Dai M Org Lett. 2015 May 1;17(9):2186-9. doi: 10.1021/acs.orglett.5b00782. Epub 2015 Apr 17.
The first copper-catalyzed ring-opening electrophilic trifluoromethylation and trifluoromethylthiolation of cyclopropanols to form Csp3-CF3 and Csp3-SCF3 bonds have been realized. These transformations are efficient for the synthesis of β-CF3- and β-SCF3-substituted carbonyl compounds that are otherwise challenging to access. The reaction conditions are mild and tolerate a wide range of functional groups. Application to a concise synthesis of LY2409021, a glucagon receptor antagonist that is used in clinical trials for type 2 diabetes mellitus, is reported as well.
3.Treatment with LY2409021, a glucagon receptor antagonist, increases liver fat in patients with type 2 diabetes.
Guzman CB;Zhang XM;Liu R;Regev A;Shankar S;Garhyan P;Pillai SG;Kazda C;Chalasani N;Hardy TA Diabetes Obes Metab. 2017 Nov;19(11):1521-1528. doi: 10.1111/dom.12958. Epub 2017 Jun 8.
AIMS: ;To evaluate whether treatment with LY2409021, a novel, selective glucagon receptor antagonist, is associated with changes in hepatic fat and other safety variables related to the benefit-risk profile for chronic use in patients with type 2 diabetes (T2D).;METHODS: ;Safety and efficacy were assessed in patients with T2D taking metformin and sulphonylurea who were randomized to LY2409021 20 mg (n = 65), placebo (n = 68), or sitagliptin 100 mg (n = 41). Key endpoints included change from baseline to month 6 in hepatic fat fraction (HFF), assessed by magnetic resonance imaging; hepatic aminotransferases; blood pressure; lipid profile; fasting plasma glucose; and glycated haemoglobin (HbA1c).;RESULTS: ;A significant increase in HFF was seen with LY2409021 vs sitagliptin (least squares [LS] mean difference 3.72%; P < .001) and placebo (4.44%; P < .001), accompanied by significant elevations in alanine aminotransferase levels with LY2409021 vs sitagliptin (6.8 U/L; P = .039) and vs placebo (10.7 U/L; P < .001). No patients had concomitant elevations in bilirubin levels. LY2409021 treatment showed significant HbA1c reductions vs placebo (LS mean difference -0.77%; P < .001) but not sitagliptin (-0.
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CAS 1488363-78-5 Adomeglivant

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