1. GPCR/G Protein Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. BIIE-0246 hydrochloride

BIIE-0246 hydrochloride  (Synonyms: AR-H 053591 hydrochloride)

目录号: HY-101986A 纯度: ≥99.0%
COA 产品使用指南

BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) 是一种有效的选择性神经 Y 受体2 NPY2R 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。

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BIIE-0246 hydrochloride Chemical Structure

BIIE-0246 hydrochloride Chemical Structure

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Other Forms of BIIE-0246 hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

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]

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

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]

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

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

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 40 mg/mL (超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
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浓度
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体积
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分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

参考文献

BIIE-0246 hydrochloride 相关分类

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BIIE-0246 hydrochloride
目录号:
HY-101986A
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