氯雷他定, 组胺 H1 受体拮抗剂

H1 receptor Selective Inhibitors | Agonists | Antagonists

10mM in DMSO

CAS编号: 79794-75-5(DMSO)
分子式: C₂₂H₂₃ClN₂O₂
分子量: 382.88

有货

库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
L408535-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester
规格或纯度	10mM in DMSO
英文名称	Loratadine (SCH29851)
生化机理	氯雷他定（SCH29851）是一种组胺 H1 受体拮抗剂，用于治疗过敏症。也是 B(0)AT2 的选择性抑制剂，IC50 为 4 μM。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	拮抗剂
作用机制	组胺 H1 受体拮抗剂
产品介绍	Loratadine是一种选择性的，逆向外周组胺H1受体激动剂，IC50大于32 μM。A peripheral histamine H1 receptor agonist. Information Loratadine (SCH29851) is ahistamine H1 receptorantagonist, used to treat allergies. Also acts as a selective inhibitor ofB(0)AT2withIC50of 4 μM. In vitro 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. In vivo Cell Data cell lines：A549 cell line, Ovcar-3 cell line Concentrations： Incubation Time： Powder Purity:≥99%

产品属性

IC50	H1 receptor, : ; B(0)AT2, IC50: 4 μM
ALogP	5
hba_count	3
Rotatable Bond	2

关联靶点（人）

CYP2C19 Tchem 细胞色素 P450 2C19(Cytochrome P450 2C19) (0 活性数据)

点击查看靶蛋白信息： CYP2C19

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

SLC6A15 Tchem 钠依赖性中性氨基酸转运体B(0)AT2(Sodium-dependent neutral amino acid transporter B(0)AT2) (0 活性数据)

点击查看靶蛋白信息： SLC6A15

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HRH1 Tclin 组胺 H1 受体(Histamine H1 receptor) (0 活性数据)

点击查看靶蛋白信息： HRH1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

KCNH2 Tclin 钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2) (0 活性数据)

点击查看靶蛋白信息： KCNH2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

Canonical SMILES	CCOC(=O)N1CCC(CC1)=C2C3=C(CCC4=C2N=CC=C4)C=C(Cl)C=C3
分子量	382.88
Reaxy-Rn	4273483
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4273483&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 75 mg/mL (254.74 mM); Ethanol: 75 mg/mL (254.74 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	17
DMSO(mM) Max Solubility	44.4
Water(mg / mL) Max Solubility	<1