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Loratadine(Loratidine SCH 29851)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Loratadine(Loratidine SCH 29851)图片
CAS NO:79794-75-5
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)382.88
FormulaC22H23ClN2O2
CAS No.79794-75-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 17 mg/mL (44.4 mM)
Water: <1 mg/mL
Ethanol: 77 mg/mL (201.1 mM)
Solubility (In vivo)Chemical Name: ethyl 4-(8-chloro-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridin-11-ylidene)piperidine-1-carboxylate
InChi Key: JCCNYMKQOSZNPW-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3
SMILES Code: CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
SynonymsSCH29851; Loratadine; Claritin; Loratidine; Clarityn; Alavert; Loratadine; Sch 29851; Sch-29851; Sch29851
实验参考方法
In Vitro

In vitro activity: Loratadine is identified as a selective inhibitor of B(0)AT2 with an IC50 of 4 μM while being less active or inactive against several other members of the SLC6 family. Loratadine concentration-dependently inhibits the release of histamine and LTC4 when preincubating before Der p 1 antigen or anti-Fc epsilon RI challenge in human Fc epsilon RI+ cells. Loratadine (0.1 mM) also inhibits (10-40%) histamine, LTC4, and PGD2 release from purified HLMC (16-68%) activated by anti-Fc epsilon RI. Loratadine causes concentration-dependent inhibition (10-40%) of histamine, tryptase, LTC4, and PGD2 release from purified HSMC (24-72%) immunologically challenged with anti-Fc epsilon RI. Loratadine inhibits significantly IL-6 and IL-8 secretion induced by histamine with a more powerful efficiency of the active metabolite in human umbilical vein endothelial cells (HUVEC). Loratadine blocks hKv1.5 channels in a concentration-, voltage-, time- and use-dependent manner but only at concentrations much higher than therapeutic plasma levels in man in Ltk- cells transfected with the gene encoding hKv1.5 channels. Loratadine inhibits rhinovirus-induced ICAM-1 upregulation in both primary bronchial or transformed (A549) respiratory epithelial cells. Loratadine also inhibits ICAM-1 mRNA induction caused by rhinovirus infection in a dose-dependent manner, and they completely inhibits rhinovirus-induced ICAM-1 promoter activation.


Cell Assay: Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of>32 μM. Loratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells.

In Vivo
Animal model
Formulation & Dosage
ReferencesJ Med Chem. 2014 Nov 26;57(22):9473-9; Clin Exp Allergy. 1997 May;27(5):559-67.