Levocabastine hydrochloride|79547-78-7|(R 50547 hydrochloride)-陌孚医药/Medlife

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Levocabastine hydrochloride (Synonyms: R 50547 hydrochloride)

目录号: PL07774 纯度: ≥99.0%

CAS No. :79547-78-7

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中文名称	Levocabastine hydrochloride
中文别名	盐酸左卡巴斯丁;盐酸左卡巴斯汀;3-羟基酪氨酸;盐酸左卡巴司丁;盐酸左卡巴斯汀 EP标准品;盐酸左卡巴斯汀 USP标准品;左旋多巴;3-(3,4-二羟基苯基)-L-丙氨酸;L-Β-(3,4-二羟基苯基)初油氨基酸;左卡巴斯汀,用于系统适应性1 EP标准品
英文名称	Levocabastine hydrochloride
英文别名	Levocabastine Hydrochloride;(3S,4R)-Cabastine;(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid,hydrochloride;(3S,4R)-Cabastine Hydrochloride;LEVOCABASTINE HCL;levocabastin;Levocabastine;levocobastine;Levophta;Livostin;R 50,547;UNII-124XMA6YEI;Levostin;[3S-[1(cis),3α,4β]]-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid;R50547;Levocabastine hydrochloride
Cas No.	79547-78-7
分子式	C₂₆H₂₉FN₂O₂^.ClH
分子量	456.98
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

Levocabastine (R 50547) hydrochloride 是一种强效选择性组胺 H1 受体拮抗剂。Levocabastine hydrochloride 也是一种选择性、高亲和力的神经降压素受体亚型 2 (NTR2) 拮抗剂，对 mNTR2 的 K_i 值为 17 nM。Levocabastine hydrochloride 可作为 VLA-4 拮抗剂，干扰过敏性结膜炎 (AC) 结膜嗜酸性粒细胞的浸润。

生物活性

Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a K i of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).

性状

Solid

IC50 & Target[1][2]

H1 Receptor NTR2 17 nM (Ki)

体外研究(In Vitro)

Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC50 of 406.2μm.
Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) hydrochloride inhibits α4β1 integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits α4β1 integrindependent adhesion of Jurkat cells to VCAM-1 with an IC50 of 395.6 μM, and the adhesion of EoL-1 cells with an IC50 of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC50=443.7 μM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) hydrochloride inhibits the virus-induced airway hyperresponsiveness.
Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior.
Levocabastine (500 μg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4.
has not independently confirmed the accuracy of these methods. They are for reference only.

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)

ClinicalTrial

参考文献

[1]. Folkerts G, et, al. Virus-induced airway hyperresponsiveness in the guinea-pig: possible involvement of histamine and inflammatory cells. Br J Pharmacol. 1993 Apr;108(4):1083-93.
[2]. Yamauchi R, et, al. Effect of beta-lactotensin on acute stress and fear memory. Peptides. 2006 Dec;27(12):3176-82.

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

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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