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

Levocabastine hydrochloride  (Synonyms: R 50547 hydrochloride)

目錄號: HY-14277A 純度: 99.3%
COA 產(chǎn)品使用指南

Levocabastine (R 50547) hydrochloride 是一種強效選擇性組胺 H1 受體拮抗劑。Levocabastine hydrochloride 也是一種選擇性、高親和力的神經(jīng)降壓素受體亞型 2 (NTR2) 拮抗劑，對 mNTR2 的 Ki 值為 17 nM。Levocabastine hydrochloride 可作為 VLA-4 拮抗劑，干擾過敏性結(jié)膜炎 (AC) 結(jié)膜嗜酸性粒細(xì)胞的浸潤。

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Levocabastine hydrochloride Chemical Structure

Levocabastine hydrochloride Chemical Structure

CAS No. : 79547-78-7

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1 mg ￥1000
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5 mg ￥2700
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Other Forms of Levocabastine hydrochloride:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

-20°C, sealed storage, away from moisture

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

純度 & 產(chǎn)品資料

純度: 99.3%

參考文獻(xiàn)

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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.

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產(chǎn)品名稱：
Levocabastine hydrochloride
目錄號：
HY-14277A
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