Bioactivity | LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research[1]. | ||||||||||||
Invitro | In vitro, LGD-6972 binds competitively to glucagon receptor (GCGR) with high affinity and selectivity, suppressing both cAMP and glucose production[1]. | ||||||||||||
In Vivo | 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]. | ||||||||||||
Name | LGD-6972 | ||||||||||||
CAS | 1207989-09-0 | ||||||||||||
Formula | C43H46N2O5S | ||||||||||||
Molar Mass | 702.90 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |