LGD-6972( LGD6972 | RVT 1502 )

Catalog No. M10771 CAS No. 1207989-09-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

LGD-6972
Note

Research use only, not for human use.
Brief Description

LGD-6972 (RVT 1502) is a novel potent, selective, orally bioavailable glucagon receptor (GCGR) antagonist.
Description

LGD-6972 (RVT 1502) is a novel potent, selective, orally bioavailable glucagon receptor (GCGR) antagonist; binds competitively to GCGR with high affinity and selectivity, suppressing both cAMP and glucose production in vitro; reduces acute glucagon-stimulated hyperglycaemia as well as the hyperglycaemia observed in diabetic mouse models in vivo.Diabetes Phase 2 Clinical.
In Vitro

In vitro, LGD-6972 binds competitively to glucagon receptor (GCGR) with high affinity and selectivity, suppressing both cAMP and glucose production.
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.
Synonyms

LGD6972 | RVT 1502
Pathway

GPCR/G Protein
Target

Glucagon Receptor
Recptor

Glucagon Receptor
Research Area

Metabolic Disease
Indication

Diabetes

CAS Number

1207989-09-0
Formula Weight

702.9008
Molecular Formula

C43H46N2O5S
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 31 mg/mL
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
Chemical Name

Ethanesulfonic acid, 2-[[4-[(2R)-2-[4'-(1,1-dimethylethyl)[1,1'-biphenyl]-4-yl]-3-oxo-3-[(2',4',6'-trimethyl[1,1'-biphenyl]-4-yl)amino]propyl]benzoyl]amino]-

1. Vajda EG, et al. Diabetes Obes Metab. 2017 Jan;19(1):24-32. 2. Vajda EG, et al. Diabetes. 2012;61(suppl 1):A252. Abstract.

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