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Purity: ≥98%
LGD-6972 (LGD6972; MB-11262) is a novel and orally bioavailable glucagon receptor antagonist with the potential to be used for treating type 2 diabetes (T2DM). In subjects with type 2 diabetes and those in good health, its linear plasma pharmacokinetics are consistent with a once-daily dosage. Additionally, it lowers postprandial plasma glucose levels. There are dose-dependent rises in fasting plasma glucagon, but in T2DM subjects, glucagon levels fall and insulin levels rise following an oral glucose load. The reduction in glucose levels observed in both T2DM patients and healthy individuals was linked to LGD-6972's inhibition of glucagon action. This effect was significant enough to forecast improvements in glycaemic control in T2DM patients who received longer treatment durations. Continued clinical development of LGD-6972 is supported by its safety and pharmacological profile after 14 days of dosing.
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| Additional Infomation |
LGD-6972 is under investigation in clinical trial NCT01919684 (Study to Evaluate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of LGD-6972 in Healthy Subjects and Subjects With Type 2 Diabetes Mellitus).
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| Molecular Formula |
C43H46N2O5S
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| Molecular Weight |
702.9
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| Exact Mass |
702.312
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| Elemental Analysis |
C, 73.48; H, 6.60; N, 3.99; O, 11.38; S, 4.56
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| CAS # |
1207989-09-0
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| Related CAS # |
1207989-22-7 (sodium); 1207989-09-0 (free)
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| PubChem CID |
44625560
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| Appearance |
Solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.616
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| LogP |
8.45
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
51
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S(C([H])([H])C([H])([H])N([H])C(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])[C@@]([H])(C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])C1C(C([H])([H])[H])=C([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])[H])=O)C1C([H])=C([H])C(=C([H])C=1[H])C1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O)(=O)(=O)O[H]
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| InChi Key |
HKJMCBYPVCGZFB-LDLOPFEMSA-N
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| InChi Code |
InChI=1S/C43H46N2O5S/c1-28-25-29(2)40(30(3)26-28)35-17-21-38(22-18-35)45-42(47)39(27-31-7-9-36(10-8-31)41(46)44-23-24-51(48,49)50)34-13-11-32(12-14-34)33-15-19-37(20-16-33)43(4,5)6/h7-22,25-26,39H,23-24,27H2,1-6H3,(H,44,46)(H,45,47)(H,48,49,50)/t39-/m1/s1
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| Chemical Name |
2-[[4-[(2R)-2-[4-(4-tert-butylphenyl)phenyl]-3-oxo-3-[4-(2,4,6-trimethylphenyl)anilino]propyl]benzoyl]amino]ethanesulfonic acid
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.96 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 20.8 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: ≥ 2.08 mg/mL (2.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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: ≥ 2.08 mg/mL (2.96 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 | 1.4227 mL | 7.1134 mL | 14.2268 mL | |
| 5 mM | 0.2845 mL | 1.4227 mL | 2.8454 mL | |
| 10 mM | 0.1423 mL | 0.7113 mL | 1.4227 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02250222 | Completed | Drug: LGD-6972 Drug: Placebo (Captisol ®) |
Type 2 Diabetes Mellitus | Ligand Pharmaceuticals | October 2014 | Phase 1 |
| NCT02672839 | Completed | Drug: LGD-6972 Solution Drug: LGD-6972 Capsules |
Type 2 Diabetes Mellitus (T2DM) |
Ligand Pharmaceuticals | February 2016 | Phase 1 |
| NCT01919684 | Completed | Drug: LGD-6972 Drug: Placebo (Captisol®) |
Type 2 Diabetes Mellitus | Ligand Pharmaceuticals | November 2013 | Phase 1 |
| NCT02851849 | Completed | Drug: LGD-6972-5 mg Drug: LGD-6972-10 mg Drug: LGD-6972-15 mg |
Type 2 Diabetes Mellitus | Ligand Pharmaceuticals | September 2016 | Phase 2 |
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