Velneperit (S2367)

An antagonist of NPY receptor Y5

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库存: 现货

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促销价

数量
5mg

￥987.00

790.00

- +
10mg

￥1625.00

1300.00

- +
50mg

￥6037.00

4830.00

- +
100mg

￥10250.00

8200.00

- +

已选 0 种 0 瓶

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Background

Velneperit is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y₅ (K_i = 5.3 nM).¹ It is selective for Y₅ over Y₁, Y₂, and Y₄ receptors, as well as a panel of 44 receptors, ion channels, transporters and enzymes, at 10 ?M. Velneperit inhibits NPY-induced decreases in forskolin-induced cAMP production in CHO-K1 cells expressing the human Y₅ receptor (IC₅₀ = 169 nM). In vivo, velneperit (50 mg/kg) suppresses Y₅ agonist-induced increases in food intake in high-fat diet-induced obese (DIO) mice. It also reduces body weight gain and suppresses food intake in DIO mice.

1.Fukasaka, Y., Nambu, H., Tanioka, H., et al.An insurmountable NPY Y5 receptor antagonist exhibits superior anti-obesity effects in high-fat diet-induced obese miceNeuropeptides7055-63(2018)