BIIE-0246 hydrochloride  (Synonyms: AR-H 053591 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]PYY_3-36. 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].

BIIE-0246 hydrochloride (1 µM; 24 h) decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated (10, 100 ng/mL) in mouse podocytes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BIIE-0246 hydrochloride (1.3 mg/kg; I.p.; daily for 2 or 4.5 weeks) prevents diet-induced obesity in OE-NPYDβH mice, but enhances obesity in WT Mice^[1].
BIIE-0246 hydrochloride (10 µg/day; i.p.; daily for 14 days) reduces albuminuria in ADR (adriamycin) nephropathy^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

C₄₉H₅₇N₁₁O₆.xHCl

Solid

White to off-white

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]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]