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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: ≥99.0%
COA 產(chǎn)品使用指南 技術支持

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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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥1000
In-stock
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

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)

左卡巴斯?。?-1000微摩爾；HEK-293細胞）鹽酸鹽能夠以濃度依賴性方式抑制125I-FN與SPA珠結(jié)合的α4β1整合素的結(jié)合，其半數(shù)抑制濃度（IC50）為406.2微摩爾[3]。
左卡巴斯?。?-1000微摩爾；處理30分鐘；Jurkat細胞和EoL-1細胞）鹽酸鹽在體外抑制由α4β1整合素/VCAM-1介導的細胞粘附。對于Jurkat細胞，左卡巴斯汀對α4β1整合素依賴性粘附到VCAM-1的抑制作用的IC50值為395.6微摩爾；而對于EoL-1細胞，該值為403.6微摩爾。此外，左卡巴斯汀還能抑制人嗜酸性粒細胞對包被有VCAM-1的孔的粘附，其IC50為443.7微摩爾[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

左卡巴斯汀 (R 50547；0.25 mg/kg；腹腔注射；每天兩次，持續(xù)五天；患有副流感 3 (PI-3) 病毒的豚鼠) 鹽酸鹽可抑制病毒引起的氣道高反應性[1]。
鹽酸左卡巴斯汀 (0.05 mg/kg；腹腔注射；一次；雄性 C57BL/6J 小鼠) 阻斷β-LT 對小鼠行為的抗應激作用[2]。
左卡巴斯汀 (500 μg/眼；滴眼液；一次；卵清蛋白致敏的豚鼠) 鹽酸鹽誘導過敏性結(jié)膜炎 (AC) 和結(jié)膜 VLA-4 顯著增加[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 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

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