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| 25mg |
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Purity: ≥98%
Adomeglivant (formerly known as LY-2409021) is a novel, potent and selective glucagon receptor antagonist that is being investigated in clinical trial for type 2 diabetes mellitus. Adomeglivant (LY2409021) lowers blood sugar levels in both type 2 diabetics and healthy individuals. Patients with type 2 diabetes respond well to glucagon signalling blockade, which significantly lowers fasting and postprandial glucose levels with little hypoglycemia but causes reversible increases in aminotransferases. For patients with type 2 diabetes, LY2409021's inhibition of glucagon signaling is a promising potential treatment. To fully assess the benefits and risks, longer clinical trials should be conducted.
| Targets |
Glucagon Receptor
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|---|---|
| ln Vitro |
Adomeglivant cannot block the cAMP-increasing effect of pancreatic islets [2]. Adomeglivant exhibits high resistance to group B GPCRs and resonates with the oscillatory binding motif potential in GluR, GLP-1R and GIP-R [2].
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| ln Vivo |
Adomeglivant (5 mg/kg; ip) completely eliminates the hypertensive effects of CNO (clozapine-N-oxide) in Avpires-Cre+ electrodes. (CNO is a cardiovascular drug stimulant that can induce hM3Dq-induced membrane myocardial infarction and increase the firing rate of hM3Dq-expressing arginine vasopressin (AVP) neurons) [3] Animal model: Avpires-Cre+ small Rat [3] Dosage: 5 mg/kg Administration method: intraperitoneal injection, 30 minutes before CNO. Results: The hyperglycemic effect of CNO was completely eliminated.
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| References |
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| Molecular Formula |
C32H36F3NO4
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|---|---|
| Molecular Weight |
555.6278
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| Exact Mass |
555.26
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| Elemental Analysis |
C, 69.17; H, 6.53; F, 10.26; N, 2.52; O, 11.52
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| CAS # |
1488363-78-5
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| Related CAS # |
872260-47-4 (racemic); 488363-78-5 (S-isomer); 872260-19-0 (R-isomer)
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=CC(=CC(=C1C2=CC=C(C=C2)C(C)(C)C)C)O[C@@H](CCC(F)(F)F)C3=CC=C(C=C3)C(=O)NCCC(=O)O
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| InChi Key |
FASLTMSUPQDLIB-MHZLTWQESA-N
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| 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
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| Chemical Name |
3-[[4-[(1S)-1-[4-(4-tert-butylphenyl)-3,5-dimethylphenoxy]-4,4,4-trifluorobutyl]benzoyl]amino]propanoic acid
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| Synonyms |
LY-2409021; LY2409021; LY 2409021
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~180 mM)
Ethanol: ~100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.50 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7998 mL | 8.9988 mL | 17.9976 mL | |
| 5 mM | 0.3600 mL | 1.7998 mL | 3.5995 mL | |
| 10 mM | 0.1800 mL | 0.8999 mL | 1.7998 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Time course for LS mean (90% CI) change from baseline in HbA1clevel by week and treatment with LY2409021 or placebo over the 12-week phase 2a study (A) and 24-week phase 2b study (B) treatment periods.Time course for LS mean (95% CI) change from baseline in fasting glucose level by week and treatment with LY2409021 or placebo over the 12-week phase 2a study (C) and 24-week phase 2b study (D) treatment periods. *P< 0.001 and †P< 0.05, compared with placebo. **P= 0.05, compared with placebo. Diabetes Care. 2016 Jul;39(7):1241-9. |
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 LS mean (95% CI) change from baseline in SMBG level by time point and treatment with LY2409021 or placebo at end point week 12 (phase 2a study) (A) and week 24 (phase 2b study) (B).
A: Time course for mean (±SE) change from baseline in ALT level (units/L) by week and treatment with LY2409021 or placebo over the 12-week phase 2a study treatment period. The ULNs for ALT level were 43 units/L (dashed line, male) and 34 units/L (dotted line, female).B: Time course for LS mean change (95% CI) from baseline in ALT level (units/L) by week and treatment with LY2409021 or placebo over the 24-week phase 2b study treatment period.Diabetes Care. 2016 Jul;39(7):1241-9. |
 A: Time course for mean (±SE) change from baseline in fasting glucagon level (pmol/L) by week and treatment with LY2409021 or placebo over the 12-week phase 2a study treatment period.B: Time course for LS mean (95% CI) change from baseline in fasting glucagon level (pmol/L) by week and treatment with LY2409021 or placebo over the 24-week phase 2b study treatment period.C: Time course for mean (±SE) change from baseline in fasting total GLP-1 level (pmol/L) by week and treatment with LY2409021 or placebo over the 12-week phase 2a study treatment period.D: Time course for LS mean (95% CI) change from baseline in fasting total GLP-1 level (pmol/L) by week and treatment with LY2409021 or placebo over the 24-week phase 2b study treatment period.Diabetes Care. 2016 Jul;39(7):1241-9. |
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