左西替利嗪

• 常用名: 左西替利嗪
• 英文名: Levocetirizine
• CAS号: 130018-77-8
• 分子量: 388.888
• 密度: 1.2±0.1 g/cm3
• 沸点: 542.1±45.0 °C at 760 mmHg
• 分子式: C₂₁H₂₅ClN₂O₃
• 熔点: 205-208°C (dec.)
• 闪点: 281.6±28.7 °C

左西替利嗪用途

Levocetirizine ((R)-Cetirizine) 是第三代 peripheral H1-receptor 拮抗剂。Levocetirizine 是一种抗组胺药,是 Cetirizine 的 R 对映体。Levocetirizine 对组胺 H1-受体的亲和力高于 (S)-Cetirizine,并且可有效治疗变应性鼻炎和慢性特发性荨麻疹。

左西替利嗪名称

• 中文名: 左西替利嗪
• 英文名: Levocetirizine
• 中文别名: (R)-西替利嗪二盐酸盐 | 2-[2-[4-[(4-氯苯基)-苯基甲基]哌嗪-1-基]乙氧基]乙酸

左西替利嗪生物活性

• 描述: Levocetirizine ((R)-Cetirizine) 是第三代 peripheral H1-receptor 拮抗剂。Levocetirizine 是一种抗组胺药,是 Cetirizine 的 R 对映体。Levocetirizine 对组胺 H1-受体的亲和力高于 (S)-Cetirizine,并且可有效治疗变应性鼻炎和慢性特发性荨麻疹。
• 相关类别:
  研究领域 >> 内分泌
• 靶点实验:

  H1 receptor

• 体内研究: 左西替利嗪(0.4 mg/kg；口服；雄性Sprague-Dawley大鼠)治疗显示Cmax,AUC0-t,AUC0-∞和t1/2分别为0.34μg/mL,3.26μg h/mL,3.67μgh/mL和Sprague-Dawley大鼠分别为2.34小时[1]。动物模型：30只雄性Sprague-Dawley大鼠(8周龄；200-250g)[1]剂量：0.4mg/kg给药：口服给药(药代动力学分析)结果：Cmax,AUC0-t,AUC0-∞和t1/2分别为0.34μg/mL,3.26μg h/mL,3.67μgh/mL和2.34小时。
• 参考文献:

  [1]. Lohar P, et al. Simultaneous bioanalysis and pharmacokinetic interaction study of acebrophylline, levocetirizine and pranlukast in Sprague-Dawley rats. Biomed Chromatogr. 2019 Dec;33(12):e4672.

左西替利嗪物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 542.1±45.0 °C at 760 mmHg
• 熔点: 205-208°C (dec.)
• 分子式: C₂₁H₂₅ClN₂O₃
• 分子量: 388.888
• 闪点: 281.6±28.7 °C
• 精确质量: 388.155365
• PSA: 53.01000
• LogP: 2.16
• InChIKey: ZKLPARSLTMPFCP-OAQYLSRUSA-N
• SMILES: O=C(O)COCCN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1
• 外观性状: 白色至米白色粉末或晶体
• 蒸汽压: 0.0±1.5 mmHg at 25°C
• 折射率: 1.589
• 储存条件: -20°C Freezer

左西替利嗪安全信息

• 危害码 (欧洲): Xn
• 海关编码: 2933599090

左西替利嗪海关

• 海关编码: 2933599090
• 中文概述: 2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
• Summary: 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

左西替利嗪靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020);... 来源：ChEMBL 靶标：Staphylococcus aureus External Id：CHEMBL4296184

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); ... 来源：ChEMBL 靶标：Klebsiella pneumoniae External Id：CHEMBL4296186

共154条，当前第1页，共16页

1

2

3

4

5

左西替利嗪英文别名

• Levocetirizine [INN]
• vardenafilH
• Vivanza
• MFCD04112703
• levocarnitine
• (2-(4-((R)-(4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetic Acid
• (2-{4-[(R)-(4-Chlorophenyl)(phenyl)methyl]-1-piperazinyl}ethoxy)acetic acid
• (2-{4-[(R)-(4-Chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
• Vardenafil
• (-)-Cetirizine
• levocetirizinum
• (R)-Cetirizine
• Levocetirizine