1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. J-113397

J-113397 是第一个有效的选择性的非肽基 ORL1 receptor 拮抗剂 (Ki: 克隆人源 ORL1=1.8 nM),对其他阿片受体无任何激动作用。

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J-113397 Chemical Structure

J-113397 Chemical Structure

CAS No. : 256640-45-6

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1 mg ¥1500
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5 mg ¥4480
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Customer Review

Other Forms of J-113397:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors[1].

IC50 & Target

NOP Receptor/ORL1

1.8 ± 0.24 nM (Ki)

κ Opioid Receptor/KOR

640 ± 87 nM (Ki)

μ Opioid Receptor/MOR

1000 ± 160 nM (Ki)

δ Opioid Receptor/DOR

>10000 nM (Ki)

体外研究
(In Vitro)

J-113397 (0-500 nM) inhibits NociceptinNociceptin/orphanin FQ (HY-P0183)-stimulated [35S]GTPγS binding to CHO cells expressing ORL1 (CHO-ORL1) but had no effect on [35S]GTPγS binding by itself[1].

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

Cell Viability Assay[1]

Cell Line: CHO-ORL1 cells
Concentration: 0, 0.1, 1, 10, 100, 200, 500 nM
Incubation Time: 10 min
Result: Inhibited nociceptin/orphanin FQ-stimulated [35S]guanosine 5′-O-(γ-thio)triphosphate (GTPγS) binding to Chinese Hamster Ovary (CHO) cells expressing ORL1 (CHO-ORL1) with an IC50 value of 5.3 nM but had no effect on [35S]GTPγS binding by itself.
体内研究
(In Vivo)

J-113397 (0-30 mg/kg; subcutaneously (s.c.); once) dose-dependently inhibits hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of NociceptinNociceptin/orphanin FQ (HY-P0183) in a tail-flick test with mice[1].

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

Animal Model: Male ICR mice (15–25 g)[1]
Dosage: 0, 3, 10, 30 mg/kg
Administration: Subcutaneously (s.c.), 10 min prior to administering 0.1 nmol nociceptin/orphanin FQ to the mice
Result: Dose-dependently inhibited hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of nociceptin/orphanin FQ in a tail-flick test with mice.
分子量

399.57

Formula

C24H37N3O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 2 mg/mL (5.01 mM; 超声加热助溶; 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 2.5027 mL 12.5135 mL 25.0269 mL
5 mM 0.5005 mL 2.5027 mL 5.0054 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 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

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5027 mL 12.5135 mL 25.0269 mL 62.5673 mL
5 mM 0.5005 mL 2.5027 mL 5.0054 mL 12.5135 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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Inquiry Information

产品名称:
J-113397
目录号:
HY-114072
需求量: