5'-Guanidinonaltrindole hydrochloride 5'-GNTI hydrochloride|cas:351183-88-5|西域试剂

5'-Guanidinonaltrindole hydrochloride 5'-GNTI hydrochloride

产品编号：Bellancom-107748| CAS NO：351183-88-5| 分子式：C₂₇H₃₁Cl₂N₅O₃| 分子量：544.47

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-107748		￥5600.00	杭州北京（现货）

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5'-Guanidinonaltrindole hydrochloride 5'-GNTI hydrochloride

产品介绍

5'-Guanidinonaltrindole (5'-GNTI) hydrochloride 是一种高选择性的、有效的 κ-opioid receptor 拮抗剂，对人 κ-opioid 受体的 K_i 为 0.18 nM。

生物活性

5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a K_i of 0.18 nM for human κ-opioid receptor.

体外研究

5'-Guanidinonaltrindole (5'-GNTI) also binds to human μ- and δ-opioid receptors with K_is of 36.9±2.3 nM and 70.0±0.3 nM, respectively.
5'-Guanidinonaltrindole is most effective at κ-opioid receptors (pA₂=10.4±0.10), with substantially lower antagonist potency at μ-opioid (pA₂=8.49±0.09) and δ-opioid receptors (pA₂=7.81±0.06).

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

体内研究

5'-Guanidinonaltrindole (5'-GNTI) (0.03-3 mg/kg; s.c.; once) induces scratching in mice.

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

Animal Model:	Male Swiss-Webster mice
Dosage:	0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:	Subcutaneous injection, once
Result:	Induced scratching, the scratch A₅₀ value was calculated to be 0.17 mg/kg.

体内研究

5'-Guanidinonaltrindole (5'-GNTI) (0.03-3 mg/kg; s.c.; once) induces scratching in mice.

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

Animal Model:	Male Swiss-Webster mice
Dosage:	0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration:	Subcutaneous injection, once
Result:	Induced scratching, the scratch A₅₀ value was calculated to be 0.17 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (229.58 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8366 mL	9.1832 mL	18.3665 mL
5 mM	0.3673 mL	1.8366 mL	3.6733 mL
10 mM	0.1837 mL	0.9183 mL	1.8366 mL

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

参考文献