For research use only. Not for therapeutic Use.
LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research[1].
In vitro, LGD-6972 binds competitively to glucagon receptor (GCGR) with high affinity and selectivity, suppressing both cAMP and glucose production[1].
In vivo, LGD-6972 reduces acute glucagon-stimulated hyperglycaemia as well as the hyperglycaemia observed in diabetic mouse models. The pharmacological activity of LGD-6972 appears to be mediated primarily by inhibiting glucagon receptor signaling[1].
| Catalog Number | I020673 |
| CAS Number | 1207989-09-0 |
| Synonyms | 2-[[4-[(2R)-2-[4-(4-tert-butylphenyl)phenyl]-3-oxo-3-[4-(2,4,6-trimethylphenyl)anilino]propyl]benzoyl]amino]ethanesulfonic acid |
| Molecular Formula | C43H46N2O5S |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | HKJMCBYPVCGZFB-LDLOPFEMSA-N |
| SMILES | CC1=CC(=C(C(=C1)C)C2=CC=C(C=C2)NC(=O)C(CC3=CC=C(C=C3)C(=O)NCCS(=O)(=O)O)C4=CC=C(C=C4)C5=CC=C(C=C5)C(C)(C)C)C |
| Reference | [1]. Vajda EG, et al. 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. |
