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

Levocabastine  (Synonyms: R 50547)

目录号: HY-14277
产品使用指南

Levocabastine (R 50547) 是一种强效选择性组胺 H1 受体拮抗剂。Levocabastine 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 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。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Levocabastine Chemical Structure

Levocabastine Chemical Structure

CAS No. : 79516-68-0

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Levocabastine 的其他形式现货产品:

Customer Review

Other Forms of Levocabastine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Levocabastine (R 50547) 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 can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].

IC50 & Target[1][2][3]

H1 Receptor

 

α4β1

 

NTR2

17 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
28 nM
Compound: 6
Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay
Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay
[PMID: 24856674]
体外研究
(In Vitro)

Levocabastine (0-1000 μM; HEK-293 cells) 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) 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.

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) inhibits the virus-induced airway hyperresponsiveness[1].
Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) blocks anti-stress effect ofβ-LT on mouse behavior[2].
Levocabastine (500 µg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) 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 of β-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

420.52

Formula

C26H29FN2O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
Levocabastine
目录号:
HY-14277
需求量: