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. |
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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. |
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| Formula | |
| 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. |
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