5'-Guanidinonaltrindole hydrochloride|351183-88-5|(5'-GNTI hydrochloride)-陌孚医药/Medlife

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5'-Guanidinonaltrindole hydrochloride (Synonyms: 5'-GNTI hydrochloride)

目录号: PL08080 纯度: ≥98%

CAS No. :351183-88-5

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中文名称	5'-Guanidinonaltrindole hydrochloride
中文别名	[(4bS,8R,8aS,14bR)-7-(环丙基甲基)-5,6,7,8,8a,9,14,14b-八氢-1,8a-二羟基-4,8-甲桥苯并呋喃并[2,3-a]吡啶并[4,3-b]咔唑-11-基]胍二盐酸盐
英文名称	5'-Guanidinonaltrindole hydrochloride
英文别名	GNTI dihydrochloride;5'-Guanidinyl-17-(cyclopropylMethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indoloMorphinandihydrochloride
Cas No.	351183-88-5
分子式	C₂₇H₃₀Cl₂N₄O₃
分子量	529.46
包装储存	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	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.
性状	Solid
IC50 & Target[1][2]	human μ-opioid receptor 36.9 nM (Ki) human μ-opioid receptor
体外研究(In Vitro)	5-Guanidinonaltrindole (5-GNTI) also binds to human μ- and δ-opioid receptors with Kis 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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	5-Guanidinonaltrindole (5-GNTI) (0.03-3 mg/kg; s.c.; once) induces scratching in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Swiss-Webster mice
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Jones R M, et al. 5′-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. European journal of pharmacology, 2000, 396(1): 49-52. [2]. Cowan A, et al. Itching-like behavior: A common effect of the kappa opioid receptor antagonist 5′-guanidinonaltrindole and the biased kappa opioid receptor agonist 6′-guanidinonaltrindole in mice. Medicine in Drug Discovery, 2021, 11: 100097.

溶解度数据	In Vitro: DMSO : 125 mg/mL (229.58 mM; ultrasonic and warming and heat to 60°C)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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