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BIIE-0246
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BIIE-0246
CAS No. : 246146-55-4
MCE 站:BIIE-0246
产品活性:BIIE-0246 是一种有效的、非肽神经肽 Y (NPY) Y2 受体的高度选择性拮抗剂,其 IC50 值为 15 nM。
研究领域:GPCR/G Protein | Neuronal Signaling
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.
相关产品:Galanin (1-30), human | HT-2157 | SHA 68 | CGP71683 hydrochloride | RF9 | Neuropeptide Y (human) (TFA) | BIBO3304 TFA | Velneperit | Galanin (1-16), mouse, porcine, rat TFA | M40 | BIBP3226 TFA | BMS-193885 | Galanin Receptor Ligand M35 | Galantide | L 152804 | Neuropeptide Y (3-36) (human, rat) | Neuropeptide Y(29-64) | RFRP-1(human) | [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA | CYM 9484 | Galanin (1-29)(rat, mouse) | GR231118 | M1145 | Neuropeptide S(Mouse)
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