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: 99.3%
COA 产品使用指南

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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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Other Forms of Levocabastine hydrochloride:

Levocabastine hydrochloride 相关抗体

Top Publications Citing Use of Products

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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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)

Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of 125I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC50 of 406.2μm[3].
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)[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)

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[1].
Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior[2].
Levocabastine (500 µg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4[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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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.

Keywords:

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

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