BIIE-0246 hydrochloride_product_DataBase

Bioactivity	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].
Invitro	BIIE-0246 hydrochloride (1 µM; 24 h) 降低 NPY (10, 100 ng/mL) 刺激下小鼠足细胞中 p-AKT S473、P-p44/42 MAPK 的表达[3]。 Western Blot Analysis[3] Cell Line:
In Vivo	BIIE-0246 hydrochloride (1.3 mg/kg; I.p.; daily for 2 or 4.5 weeks) 可防止 OE-NPYDβH 小鼠因饮食引起的肥胖，但会增加 WT 小鼠的肥胖[1]。BIIE-0246 hydrochloride (10 µg/day; i.p.; daily for 14 days) 减少 ADR 肾病患者的白蛋白尿[3]。 Animal Model:
Name	BIIE-0246 hydrochloride
Formula	C49H57N11O6.xHCl
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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.

PeptideDB

BIIE-0246 hydrochloride

CAS: F: C49H57N11O6.xHCl W: