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BIIE-0246 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIIE-0246 hydrochloride图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AR-H 053591 hydrochloride
产品介绍
BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) 是一种有效的选择性神经 Y 受体2NPY2R拮抗剂,对大鼠 [125I]PYY3-36位点的IC50值为 15 nM。BIIE-0246 hydrochloride 在 NPY 刺激下降低 p-AKT S473、P-p44/42 MAPK 的表达。BIIE-0246 hydrochloride 减少 ADR 肾病患者的白蛋白尿。
生物活性

BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) is a potent and selectiveNPY2R (neuropeptide Y receptor 2)antagonist with anIC50value 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].

体外研究
(In Vitro)

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:Mouse podocytes
Concentration:1 μM
Incubation Time:24 h
Result:Blocked the NPY-stimulated phosphorylation of Akt and p44/42 MAPK.
体内研究
(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:Homozygous transgenic male OE-NPYDβH and WT C57Bl/6N mice[1]
Dosage:1.3 mg/kg
Administration:I.p.; daily for 2 or 4.5 weeks
Result:Increased body weight gain in both genotypes on the chow diet caused metabolic disturbances, especially in WT mice. During energy surplus (i.e., on Western diet), blocking of Y2-receptors induced obesity in WT mice and OE-NPYDβH mice showed a reduced fat mass gain, hepatic glycogen and serum cholesterol levels relative to body adiposity.
Animal Model:Male BALB/c mice[3]
Dosage:10 μg/day
Administration:I.p.; daily for 14 days
Result:Reduces albuminuria in ADR nephropathy.
Formula

C49H57N11O6.xHCl

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.