1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. JP1302

JP1302 是一种选择性的、高亲和力的 α2C 肾上腺受体 (α2C-adrenoceptor) 的拮抗剂,其对人类 α2C 受体的 Kb 值为 16 nM,Ki 为 28 nM。JP1302 具有抗抑郁和类抗精神病作用。JP1302 可用于神经精神障碍和肾功能障碍的研究。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 JP1302 dihydrochloride 通常具有更好的水溶性和稳定性。

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JP1302 Chemical Structure

JP1302 Chemical Structure

CAS No. : 80259-18-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research[1][2][3].

IC50 & Target

human α2C-adrenoceptor

28±2 nM (Ki)

human α2B-adrenoceptor

1470±130 nM (Ki)

human α2A-adrenoceptor

3150±50 nM (Ki)

rodent α2D-adrenoceptor

1700±200 nM (Ki)

体外研究
(In Vitro)

JP1302 shows about 100-fold higher affinity than for α2A or α2B[1].

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

体内研究
(In Vivo)

JP1302 (1-10 μmol/kg) decreases immobility time in the FST to a level similar to that seen with 10-30 μmol/kg of the antidepressant Desipramine (HY-B1272A)[1].
JP1302 (5 μmol/kg, once) is capable of complete reversal of the impairment in PPI induced in Sprague-Dawley rats by the psychotomimetic NMDA receptor antagonist, phencyclidine and similar results are found in Wistar rats[1].
JP1302 (3 mg/kg, IV, once) significantly ameliorates renal dysfunction[3].

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

Animal Model: Male Sprague Dawley rats (8 weeks old)[3]
Dosage: 3 mg/kg
Administration: IV, pre-treatment: administered 5 min before the induction of ischemia, post-treatment: injected 45 min after the initiation of reperfusion
Result: Significantly ameliorated renal dysfunction in the rats at 24 h after reperfusion. post-ischemic administration of JP-1302 significantly ameliorated renal dysfunction, histological damage and reduced apoptotic cells and pro-inflammatory cytokine mRNA expression.
分子量

368.47

Formula

C24H24N4

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)

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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)
× = ×
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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.

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产品名称:
JP1302
目录号:
HY-103213A
需求量: