首页工具

BIIE-0246

产品编号 T14572 CAS 246146-55-4

别名: AR-H 053591

BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist. With an IC50 of 15 nM.

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

BIIE-0246, CAS 246146-55-4

规格	价格/CNY		货期	数量
2 mg	￥ 869		5日内发货

大包装超大折扣，点击咨询

其他形式的 BIIE-0246:

BIIE 0246 hydrochloride
询价
BIIE-0246 HCl
询价

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist. With an IC50 of 15 nM.
靶点活性	NPYY2 receptor:15, Plusmn:3 nM
体外活性	Receptor binding assays in HEK 293 cells transfected with the rat Y2 receptor cDNA demonstrate that BIIE-0246 competes with high affinity (IC50=15±3 nM) against specific [125I]PYY3-36 binding sites. In contrast, BIIE-0246, at concentrations up to 10 μM, fails to compete for significant amounts of specific [125I]GR231118, [125I]hPP and [125I][Leu31, Pro34]PYY binding sites in HEK 293 cells transfected with the rat Y1, Y4 or Y5 receptor cDNA, respectively[1].
体内活性	BIIE-0246 has no significant effect on fat mass gain. In DIO, BIIE-0246 has different effects on body weight and composition depending on the genotype (treatment×genotype interaction in body weight P<0.05, in fat mass P<0.001 and in lean mass P<0.05). In DIO-NPY, BIIE-0246 inhibits fat mass gain (P=0.05). On chow diet, genetically obese NPY mice show increased gain in body weight and adiposity. Treatment with BIIE-0246 promotes body weight gain in both genotypes after 4.5 weeks, and already at 2 weeks. In DIO-WT group, post hoc analysis reveals increased body weight and fat mass gain, and a tendency to decrease lean mass gain. Interestingly, increased cholesterol levels are detected also in WT mice treated with BIIE-0246 for 2 weeks, but not in the 4.5-week cohort. In DIO-NPY mice in both treatment groups, cholesterol levels correlate positively with body fat mass (DIO-NPY vehicle P<0.01; DIO-NPY BIIE-0246 P<0.001), but not in any other group. The slope of the regression curve of cholesterol and fat mass is significantly decreased in BIIE-0246-treated DIO-NPY group when compared with vehicle-treated group[2].

别名	AR-H 053591
分子量	896.05
分子式	C49H57N11O6
CAS No.	246146-55-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (111.60 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.116 mL	5.58 mL	11.1601 mL	27.9002 mL
	5 mM	0.2232 mL	1.116 mL	2.232 mL	5.58 mL
	10 mM	0.1116 mL	0.558 mL	1.116 mL	2.79 mL
	20 mM	0.0558 mL	0.279 mL	0.558 mL	1.395 mL
	50 mM	0.0223 mL	0.1116 mL	0.2232 mL	0.558 mL
	100 mM	0.0112 mL	0.0558 mL	0.1116 mL	0.279 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. 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. 2. Liisa Ailanen, 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; 9: 319.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +