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MedKoo Cat#: 319541 | Name: Adomeglivant
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Adomeglivant, also known as LY2409021, is a potent and selective glucagon receptor antagonist. LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes. Blockade of glucagon signalling in patients with type 2 diabetes is well tolerated and results in substantial reduction of fasting and postprandial glucose with minimal hypoglycaemia, but with reversible increases in aminotransferases. Inhibition of glucagon signalling by LY2409021 is a promising potential treatment for patients with type 2 diabetes and should be evaluated in longer clinical trials to better evaluate benefits and risks.

Chemical Structure

Adomeglivant
Adomeglivant
CAS#1488363-78-5 (S-isomer)

Theoretical Analysis

MedKoo Cat#: 319541

Name: Adomeglivant

CAS#: 1488363-78-5 (S-isomer)

Chemical Formula: C32H36F3NO4

Exact Mass: 555.2596

Molecular Weight: 555.64

Elemental Analysis: C, 69.17; H, 6.53; F, 10.26; N, 2.52; O, 11.52

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,450.00 Ready to ship
1g USD 3,450.00 Ready to ship
2g USD 5,850.00 Ready to ship
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Related CAS #
872260-47-4 (racemic) 1488363-78-5 (S-isomer) 872260-19-0 (R-isomer)
Synonym
LY2409021; LY-2409021; LY 2409021; Adomeglivant
IUPAC/Chemical Name
3-(4-{(1S)-1-[(4'-tert-butyl-2,6-dimethylbiphenyl-4-yl)oxy]-4,4,4-trifluorobutyl}benzamido)propanoic acid
InChi Key
FASLTMSUPQDLIB-MHZLTWQESA-N
InChi Code
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
SMILES Code
O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C3=CC=C(C(C)(C)C)C=C3)C(C)=C2)CCC(F)(F)F)C=C1)=O
Appearance
White to off-white solid powder.
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist.
In vitro activity:
Using HEK293 cells that stably express the rat glucagon receptor (HEK293-GluR), and that were virally transduced with H188, it was confirmed that glucagon acts as a GluR agonist to raise levels of cAMP in a dose-dependent manner (Fig. 2, a1–a3). LY2409021 dose-dependently blocked this action of glucagon (Fig. 2, b1–b3), but it exerted no effect when tested alone (Fig. S2a). EC50 and IC50 values for glucagon agonist or LY2409021 antagonist action at the rat GluR were 400 pm and 1.8 μm, respectively (Fig. 2, a3 and b3). High concentrations of glucagon (1–100 nm) raised levels of cAMP in HEK293-GLP-1R cells expressing the human GLP-1R (Fig. 2, c1–c3). This action of glucagon was also blocked by LY2409021 (Fig. 2, d1–d3), whereas LY2409021 exerted no effect alone at the GLP-1 R (Fig. S2b). EC50 and IC50 values for glucagon agonist and LY2409021 antagonist actions at the GLP-1R were 4.9 nm and 1.2 μm, respectively (Fig. 2, c3 and d3). Reference: J Biol Chem. 2019 May 31;294(22):8714. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6416420/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 100.0 179.97
Ethanol 100.0 179.97
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 555.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chepurny OG, Matsoukas MT, Liapakis G, Leech CA, Milliken BT, Doyle RP, Holz GG. Nonconventional glucagon and GLP-1 receptor agonist and antagonist interplay at the GLP-1 receptor revealed in high-throughput FRET assays for cAMP. J Biol Chem. 2019 Mar 8;294(10):3514-3531. doi: 10.1074/jbc.RA118.005682. Epub 2019 Jan 8. Erratum in: J Biol Chem. 2019 May 31;294(22):8714. PMID: 30622136; PMCID: PMC6416420.
In vitro protocol:
1. Chepurny OG, Matsoukas MT, Liapakis G, Leech CA, Milliken BT, Doyle RP, Holz GG. Nonconventional glucagon and GLP-1 receptor agonist and antagonist interplay at the GLP-1 receptor revealed in high-throughput FRET assays for cAMP. J Biol Chem. 2019 Mar 8;294(10):3514-3531. doi: 10.1074/jbc.RA118.005682. Epub 2019 Jan 8. Erratum in: J Biol Chem. 2019 May 31;294(22):8714. PMID: 30622136; PMCID: PMC6416420.
In vivo protocol:
TBD
1: Hædersdal S, Lund A, Nielsen-Hannerup E, Maagensen H, van Hall G, Holst JJ, Knop FK, Vilsbøll T. The Role of Glucagon in the Acute Therapeutic Effects of SGLT2 Inhibition. Diabetes. 2020 Dec;69(12):2619-2629. doi: 10.2337/db20-0369. Epub 2020 Oct 1. PMID: 33004472; PMCID: PMC7679772. 2: Hædersdal S, Lund A, Maagensen H, Nielsen-Hannerup E, Gasbjerg LS, Rosenkilde MM, Forman JL, van Hall G, Holst JJ, Knop FK, Vilsbøll T. The glucagon receptor antagonist LY2409021 has no effect on postprandial glucose in type 2 diabetes. Eur J Endocrinol. 2022 Jan 6;186(2):207-221. doi: 10.1530/EJE-21-0865. PMID: 34863038. 3: Li Y, Ye Z, Bellman TM, Chi T, Dai M. Efficient Synthesis of β-CF3/SCF3-Substituted Carbonyls via Copper-Catalyzed Electrophilic Ring-Opening Cross-Coupling of Cyclopropanols. Org Lett. 2015 May 1;17(9):2186-9. doi: 10.1021/acs.orglett.5b00782. Epub 2015 Apr 17. PMID: 25885795; PMCID: PMC4690544. 4: Hædersdal S, Lund A, Nielsen-Hannerup E, Maagensen H, Forman JL, Holst JJ, Knop FK, Vilsbøll T. The glucagon receptor antagonist LY2409021 does not affect gastrointestinal-mediated glucose disposal or the incretin effect in individuals with and without type 2 diabetes. Eur J Endocrinol. 2022 Sep 12;187(4):507-518. doi: 10.1530/EJE-22-0291. PMID: 35977072. 5: Roth WJ, Almaya A, Kramer TT, Hofer JD. A Demonstration of Mixing Robustness in a Direct Compression Continuous Manufacturing Process. J Pharm Sci. 2017 May;106(5):1339-1346. doi: 10.1016/j.xphs.2017.01.021. Epub 2017 Jan 30. PMID: 28153598. 6: 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. Response to Comment on Kazda et al. Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies. Diabetes Care 2016;39:1241-1249. Diabetes Care. 2016 Nov;39(11):e199-e200. doi: 10.2337/dci16-0030. PMID: 27926898. 7: Agrawal S, Gupta Y. Comment on Kazda et al. Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies. Diabetes Care 2016;39:1241-1249. Diabetes Care. 2016 Nov;39(11):e198. doi: 10.2337/dc16-1340. PMID: 27926897. 8: Guzman CB, Zhang XM, Liu R, Regev A, Shankar S, Garhyan P, Pillai SG, Kazda C, Chalasani N, Hardy TA. Treatment with LY2409021, a glucagon receptor antagonist, increases liver fat in patients with type 2 diabetes. Diabetes Obes Metab. 2017 Nov;19(11):1521-1528. doi: 10.1111/dom.12958. Epub 2017 Jun 8. PMID: 28371155. 9: Kazda CM, Frias J, Foga I, Cui X, Guzman CB, Garhyan P, Heilmann C, Yang JA, Hardy TA. Treatment with the glucagon receptor antagonist LY2409021 increases ambulatory blood pressure in patients with type 2 diabetes. Diabetes Obes Metab. 2017 Aug;19(8):1071-1077. doi: 10.1111/dom.12904. Epub 2017 Mar 27. PMID: 28191913. 10: Kelly RP, Garhyan P, Raddad E, Fu H, Lim CN, Prince MJ, Pinaire JA, Loh MT, Deeg MA. Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes. Diabetes Obes Metab. 2015 Apr;17(4):414-22. doi: 10.1111/dom.12446. Epub 2015 Mar 2. PMID: 25656305. 11: 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. Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies. Diabetes Care. 2016 Jul;39(7):1241-9. doi: 10.2337/dc15-1643. Epub 2015 Dec 17. Erratum in: Diabetes Care. 2017 Jun;40(6):808. PMID: 26681715.

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