1. GPCR/G Protein Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. J-115814

J-115814 是一种有效的和选择性的神经肽 Y1 (neuropeptide Y1) 拮抗剂,其对 hY1、rY1、mY1、hY2、hY4、hY5、mY6 的 Ki 值分别为 1.4、1.8、1.9、>10000、620、6000、>10000 nM。J-115814 可抑制进食行为。

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J-115814 Chemical Structure

J-115814 Chemical Structure

CAS No. : 329716-61-2

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查看 Neuropeptide Y Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

J-115814 is a potent and selective neuropeptide Y1 antagonist with Ki values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors[1].

IC50 & Target[1]

hY1 receptor

1.4 nM (Ki)

rNPY Y1 receptor

1.8 nM (Ki)

mY1

1.9 nM (Ki)

hY4 receptor

620 nM (Ki)

hY5 receptor

6000 nM (Ki)

human Y2 receptor

>10000 nM (Ki)

mY6

>10000 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
1.4 nM
Compound: 1
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
[PMID: 19487123]
体内研究
(In Vivo)

J-115814 (0.3, 1, 3, 10 mg/kg; i.v.) 可抑制 NPY 诱导的 SD 大鼠进食[1]
J-115814 (3, 10, 30 mg/kg; i.p.) 在小鼠中显示出厌食作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: db/db and lean C57BL6 mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: I.p.
Result: Decreasesd nocturnal food intake in a dose-dependent manner.
Animal Model: SD rats[1]
Dosage: 0.3, 1, 3, 10 mg/kg
Administration: I.v.; 1 h before ICV NPY
Result: Inhibited NPY-induced feeding with significant responses at 3 and 10 mg/kg.
分子量

572.16

Formula

C29H38ClN5O3S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
J-115814
目录号:
HY-122021
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