WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 598783
CAS#: 1207989-09-0 (free)
Description: LGD-6972 is a glucagon receptor antagonist.
MedKoo Cat#: 598783
Name: LGD-6972
CAS#: 1207989-09-0 (free)
Chemical Formula: C43H46N2O5S
Exact Mass: 702.3127
Molecular Weight: 702.91
Elemental Analysis: C, 73.48; H, 6.60; N, 3.99; O, 11.38; S, 4.56
Related CAS #: 1207989-09-0 (free) 1207989-22-7 (sodium)
Synonym: LGD-6972; LGD 6972; LGD6972; MB-11262; MB 11262; MB11262;
IUPAC/Chemical Name: (R)-2-(4-(2-(4'-(tert-butyl)-[1,1'-biphenyl]-4-yl)-3-oxo-3-((2',4',6'-trimethyl-[1,1'-biphenyl]-4-yl)amino)propyl)benzamido)ethane-1-sulfonic acid
InChi Key: HKJMCBYPVCGZFB-LDLOPFEMSA-N
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
SMILES Code: O=C(NCCS(=O)(O)=O)C1=CC=C(C[C@H](C2=CC=C(C3=CC=C(C(C)(C)C)C=C3)C=C2)C(NC4=CC=C(C5=C(C)C=C(C)C=C5C)C=C4)=O)C=C1
Appearance: 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
Shelf Life: >3 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
| Biological target: | LGD-6972 is a selective and orally active glucagon receptor antagonist. |
| In vitro activity: | TBD |
| In vivo activity: | Herein this study reports that treatment with the novel, potent GRA, LGD-6972, results in dose-related decreases from baseline in FPG in subjects with T2DM. Glucose reduction was observed in fasting and postprandial states. The effects on glycaemia in T2DM subjects were accompanied by dose-related increases from baseline in fasting glucagon, total GLP-1 and active GLP-1. Reference: Diabetes Obes Metab. 2017 Jan;19(1):24-32. https://pubmed.ncbi.nlm.nih.gov/27501510/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 125.0 | 177.83 |
The following data is based on the product molecular weight 702.91 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.
| 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. Vajda EG, Logan D, Lasseter K, Armas D, Plotkin DJ, Pipkin JD, Li YX, Zhou R, Klein D, Wei X, Dilzer S, Zhi L, Marschke KB. Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2017 Jan;19(1):24-32. doi: 10.1111/dom.12752. Epub 2016 Aug 31. PMID: 27501510; PMCID: PMC5215471. |
| In vitro protocol: | TBD |
| In vivo protocol: | 1. Vajda EG, Logan D, Lasseter K, Armas D, Plotkin DJ, Pipkin JD, Li YX, Zhou R, Klein D, Wei X, Dilzer S, Zhi L, Marschke KB. Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2017 Jan;19(1):24-32. doi: 10.1111/dom.12752. Epub 2016 Aug 31. PMID: 27501510; PMCID: PMC5215471. |
1: Vajda EG, Logan D, Lasseter K, Armas D, Plotkin DJ, Pipkin JD, Li YX, Zhou R, Klein D, Wei X, Dilzer S, Zhi L, Marschke KB. Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2017 Jan;19(1):24-32. doi: 10.1111/dom.12752. Epub 2016 Aug 31. PubMed PMID: 27501510; PubMed Central PMCID: PMC5215471.
