2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Cytoskeleton
  3. Histamine Receptor Neurotensin Receptor Integrin
  4. Levocabastine hydrochloride

Levocabastine hydrochloride  (Synonyms: R 50547 hydrochloride)

目录号: HY-14277A 纯度: ≥99.0%
COA 产品使用指南 技术支持

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 Ki 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。

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Levocabastine hydrochloride Chemical Structure

Levocabastine hydrochloride Chemical Structure

CAS No. : 79547-78-7

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规格 价格 是否有货 数量
1 mg ￥1000
In-stock
5 mg ￥2700
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Other Forms of Levocabastine hydrochloride:

Levocabastine hydrochloride 相关抗体

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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NTR1 NTR2

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].

IC50 & Target[1]

H1 Receptor

 

NTR2

17 nM (Ki)

体外研究
(In Vitro)

左卡巴斯汀（0-1000微摩尔；HEK-293细胞）盐酸盐能够以浓度依赖性方式抑制125I-FN与SPA珠结合的α4β1整合素的结合，其半数抑制浓度（IC50）为406.2微摩尔[3]。
左卡巴斯汀（0-1000微摩尔；处理30分钟；Jurkat细胞和EoL-1细胞）盐酸盐在体外抑制由α4β1整合素/VCAM-1介导的细胞粘附。对于Jurkat细胞，左卡巴斯汀对α4β1整合素依赖性粘附到VCAM-1的抑制作用的IC50值为395.6微摩尔；而对于EoL-1细胞，该值为403.6微摩尔。此外，左卡巴斯汀还能抑制人嗜酸性粒细胞对包被有VCAM-1的孔的粘附，其IC50为443.7微摩尔[3]。

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

Levocabastine hydrochloride 相关抗体:
体内研究
(In Vivo)

左卡巴斯汀 (R 50547；0.25 mg/kg；腹腔注射；每天两次，持续五天；患有副流感 3 (PI-3) 病毒的豚鼠) 盐酸盐可抑制病毒引起的气道高反应性[1]。
盐酸左卡巴斯汀 (0.05 mg/kg；腹腔注射；一次；雄性 C57BL/6J 小鼠) 阻断β-LT 对小鼠行为的抗应激作用[2]。
左卡巴斯汀 (500 μg/眼；滴眼液；一次；卵清蛋白致敏的豚鼠) 盐酸盐诱导过敏性结膜炎 (AC) 和结膜 VLA-4 显著增加[3]。

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

Animal Model: Guinea-pig with Parainfluenza-3 (PI-3) virus[1]
Dosage: 0.25 mg/kg
Administration: Intraperitoneal injection; twice a day for five days
Result: Suppressed the influx of broncho-alveolar cells and increased in albumin content.
Animal Model: Male C57BL/6J mice (8-9 weeks old)[2]
Dosage: 0.05 mg/kg; 30 mg/kg (β-LT)
Administration: Intraperitoneal injection; once
Result: Blocked the anxiolytic effect ofβ-LT and decreased the number of head-dips.
Animal Model: Ovalbumin-sensitized guinea pigs[3]
Dosage: 500 µg/eye
Administration: drops eye, once
Result: Produced a noteworthy protection from allergic conjunctivitis (AC) and prevented the conjuctival elevation of VLA-4 as well as conjunctival eosinophil infiltration.
Clinical Trial
分子量

456.98

Formula

C26H30ClFN2O2
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

-20°C, sealed storage, away from moisture

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

纯度 & 产品资料

纯度: 99.3%

COA (295 KB)

产品使用指南 (1538 KB)
参考文献

Levocabastine hydrochloride 相关分类

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  • 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.

Keywords:

Levocabastine79547-78-7R 50547R50547R-50547Histamine ReceptorNeurotensin ReceptorIntegrincell adhesionallergic conjunctivitiseosinophil infiltrationairway hyperresponsiveness,Inhibitorinhibitorinhibit

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