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目錄:MedChemExpress LLC>>生化試劑>> BIIE-0246 | MCE

BIIE-0246 | MCE
  • BIIE-0246 | MCE
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更新時間:2023-06-19 09:14:27瀏覽次數(shù):74評價

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CAS 246146-55-4 純度 99.10%
分子量 896.05 分子式 C??H??N??O?
供貨周期 現(xiàn)貨 規(guī)格 10 mg
貨號 HY-101986 應(yīng)用領(lǐng)域 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥
BIIE-0246 | MCEBIIE-0246 is a potent and highly selective <b>non-peptide neuropeptide Y (NPY) Y<sub>2</sub></b> receptor antagonist, with an <b>IC<sub>50</sub></b> of 15 nM.

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BIIE-0246

CAS No. : 246146-55-4

產(chǎn)品活性:BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.

研究領(lǐng)域:GPCR/G Protein  |  Neuronal Signaling

作用靶點(diǎn):Neuropeptide Y Receptor

In Vitro: 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.

In Vivo: 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. 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-WT group, post hoc analysis reveals increased body weight and fat mass gain, and a tendency to decrease lean mass gain. In DIO-NPY, BIIE-0246 inhibits fat mass gain (P=0.05). 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, and 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.

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