BIIE-0246 (hydrochloride)

BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC50 value of 15 nM for rat [125I]PYY3-36. BIIE-0246 hydrochloride decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 hydrochloride reduces albuminuria in ADR nephropathy[1][2][3].

Product Specifications

Product Name Alternative

AR-H 053591 (hydrochloride)

UNSPSC

12352211

Target

Neuropeptide Y Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/biie-0246-hydrochloride.html

Purity

99.0

Solubility

DMSO : 40 mg/mL (ultrasonic; warming)

Smiles

O=C(N[C@H](C(NCCN1C(N(C2=CC=CC=C2)N(C3=CC=CC=C3)C1=O)=O)=O)CCCNC(N)=N)CC4(CC(N5CCN(C(C6=CC=CC=C67)C8=CC=CC=C8NC7=O)CC5)=O)CCCC4.[H]Cl.[x]

Molecular Formula

C49H57N11O6.xHCl

References & Citations

[1]Ailanen L, et al. Peripherally Administered Y2-Receptor Antagonist BIIE0246 Prevents Diet-Induced Obesity in Mice With Excess Neuropeptide Y, but Enhances Obesity in Control Mice. Front Pharmacol. 2018 Apr 5;9:319.|[2]Dumont Y, et al. BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y (2) receptor antagonist. Br J Pharmacol. 2000 Mar;129 (6) :1075-88.|[3]Lay AC, et al. A role for NPY-NPY2R signaling in albuminuric kidney disease. Proc Natl Acad Sci U S A. 2020 Jul 7;117 (27) :15862-15873.