MedKoo Cat#: 598783 | Name: LGD-6972
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Description:

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

LGD-6972 is a glucagon receptor antagonist.

Chemical Structure

LGD-6972
LGD-6972
CAS#1207989-09-0 (free)

Theoretical Analysis

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

Price and Availability

Size Price Availability Quantity
1mg USD 90.00 Ready to ship
5mg USD 210.00 Ready to ship
10mg USD 350.00 Ready to ship
25mg USD 550.00 Ready to ship
50mg USD 950.00 Ready to ship
100mg USD 1,650.00 Ready to ship
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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
More Info
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 mg/mL mM comments
Solubility
DMSO 125.0 177.83
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 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.

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. 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.