2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide Y Receptor
  4. (R)-JNJ-31020028

(R)-JNJ-31020028 是一种高亲和力，选择性，透过血脑屏障的神经肽 Y Y2 受体 (neuropeptide Y Y2 receptor) 拮抗剂，对人，大鼠和小鼠 Y2 受体的 pIC50 分别为 8.07、8.22 和 8.21。 (R)-JNJ-31020028 与人类Y1，Y4 和 Y5 受体相比，显示出大于 100 倍的选择性。(R)-JNJ-31020028 具有抗抑郁样作用。

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(R)-JNJ-31020028 Chemical Structure

(R)-JNJ-31020028 Chemical Structure

CAS No. : 1094873-17-2

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(R)-JNJ-31020028 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects[1][2].

IC50 & Target[1]

human Y2 receptor

8.07 (pIC50)

rat Y2 receptor

8.22 (pIC50)

mouse Y2 receptor

8.21 (pIC50)

体内研究
(In Vivo)

(R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) has antidepressant like effects in the olfactory bulbectomized rat (OBX) model[1].
Chronic icv administration of (R)-JNJ-31020028 at 5.6 μg/day using osmotic Alzet pump resulted in a significant decreases number of grooming events[1].
(R)-JNJ-31020028 treatment shows the Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively[1].

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

Animal Model: Male Sprague Dawley rats weighing 150-170 (OBX model)[1]
Dosage: 5.6 μg
Administration: chronic icv infusion; daily for 10 days
Result: Reduced OBX rat immobility time.
Animal Model: male Sprague-Dawley rat[2]
Dosage: 10 mg/kg
Administration: s.c. (Pharmacokinetic Analysis)
Result: The Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively.
分子量

565.68

Formula

C34H36FN5O2
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

(R)-JNJ-31020028 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

(R)-JNJ-310200281094873-17-2Neuropeptide Y ReceptorNPY receptorselectiveaffinityanti-depressantbehaviorsblood-brainbarrierCNSInhibitorinhibitorinhibit

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