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

JP1302 Chemical Structure

CAS No. : 80259-18-3

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MCE 顾客使用本产品发表的 1 篇科研文献

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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.html" class="link-product" target="_blank">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.

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (135.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7139 mL 13.5696 mL 27.1392 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL
查看完整储备液配制表
  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7139 mL 13.5696 mL 27.1393 mL 67.8481 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL 13.5696 mL
10 mM 0.2714 mL 1.3570 mL 2.7139 mL 6.7848 mL
15 mM 0.1809 mL 0.9046 mL 1.8093 mL 4.5232 mL
20 mM 0.1357 mL 0.6785 mL 1.3570 mL 3.3924 mL
25 mM 0.1086 mL 0.5428 mL 1.0856 mL 2.7139 mL
30 mM 0.0905 mL 0.4523 mL 0.9046 mL 2.2616 mL
40 mM 0.0678 mL 0.3392 mL 0.6785 mL 1.6962 mL
50 mM 0.0543 mL 0.2714 mL 0.5428 mL 1.3570 mL
60 mM 0.0452 mL 0.2262 mL 0.4523 mL 1.1308 mL
80 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8481 mL
100 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6785 mL
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
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