BIBO 3304

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BIBO 3304 是一种有效的、选择性的非肽神经肽 Y Y1 受体拮抗剂，对人和大鼠 Y1 受体的 IC50 分别为 0.38 和 0.72 nM。

BIBO 3304 is a potent, selective, nonpeptide neuropeptide Y Y1 receptor antagonist with IC50 of 0.38 and 0.72 nM for human and the rat Y1 receptor, respectively; shows low affinity for the human Y2 receptor, human and rat Y4 receptor, human and rat Y5 receptor (IC50>1,000 nM); inhibits the feeding response induced by 1 mg NPY in mice, also completely abolishes PYY-induced inhibition of insulin release in vivo.Obesity Discontinued(In Vivo):BIBO3304 TFA (30 μg; bilateral paraventricular nucleus injection) attenuates the hyperphagia following fasting.BIBO3304 TFA (15-60 μg) dose-dependently inhibits the feeding reponse mediated by 1 μg NPY.BIBO3304 TFA (0.5?μM; p.o.) significantly increases serum insulin levels.

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BIBO3304 TFA (30 μg; bilateral paraventricular nucleus injection) attenuates the hyperphagia following fasting.BIBO3304 TFA (15-60 μg) dose-dependently inhibits the feeding reponse mediated by 1 μg NPY.BIBO3304 TFA (0.5?μM; p.o.) significantly increases serum insulin levels. Animal Model:Adult male Chbb:Thom rats weighing between 300 and 340 g Dosage:30 μg Administration:bilateral paraventricular nucleus injection Result:Attenuated the hyperphagia following fasting, especially during the first 2 h of refeeding.Animal Model:7-week-old C57BL/6JAusb mice Dosage:0.5?μM Administration:p.o.Result:Significantly increased serum insulin levels.

BIBO3304

GPCR/G Protein

Neuropeptide Y Receptor

Neuropeptide Y Receptor

Metabolic Disease

Obesity

191868-14-1

643.668

C31H36F3N7O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (155.36 mM)

C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NCC3=CC=C(C=C3)CNC(=O)N

(R)-2-(2,2-diphenylacetamido)-5-guanidino-N-(4-(ureidomethyl)benzyl)pentanamide 2,2,2-trifluoroacetate

(-20℃)

With Ice Pack

≥ 2 years