Loratadine (SCH29851) - 10mM in DMSO , Histamine H1 receptor antagonist, CAS No.79794-75-5, Histamine H1 receptor antagonist

CAS: 79794-75-5 Cat. No.: L408535 Peso molecular: 382.88 Número EC: 935-907-9

GRADE & PURITY 10mM in DMSO

Synonyms

1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

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%

Specifications

Sinónimos

1-Piperidinecarboxylic acid, 4-(8-chloro-5, 6-dihydro-11H-benzo[5, 6]cyclohepta[1, 2-b]pyridin-11-ylidene)-, ethyl ester

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Loratadine (SCH29851) is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

ANTAGONIST

Mecanismo de acción

Histamine H1 receptor antagonist

Propiedades del producto

• ALogP: 5.2

Nombres e identificadores

• Isómeros SMILES: CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
• WGK Alemania: 2
• RTECS: TM6129200
• Peso molecular: 382.88
• Reaxy-Rn: 4273483
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4273483&ln=

Objetivos asociados (humanos)

CYP2C19 Tchem Cytochrome P450 2C19 (0 Activities)

Discover Target: CYP2C19

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A15 Tchem Sodium-dependent neutral amino acid transporter B(0)AT2 (0 Activities)

Discover Target: SLC6A15

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor (0 Activities)

Discover Target: HRH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (0 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 75 mg/mL (254.74 mM); Ethanol: 75 mg/mL (254.74 mM); Water: Insoluble
• Punto de fusión (°C): 137°C

Referencias

1. Xiuyan He, Wenji Hu, Yao Zu.  (2025)  Loratadine disrupts cardiovascular and swim bladder development in zebrafish.  ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY,      [PMID:40627912] [10.1016/j.ecoenv.2025.118622]

2. Jieping Zhao, Xiu Chen, Hengbin Zhang, Xiaoyan Liu, Yiwen Ma, Jianbiao Yao, Huidi Jiang, Hui Zhou.  (2023)  Quantification of nine bufadienolides of Shexiang Tongxin Dropping Pills in rat plasma and tissues using UPLC-MS/MS and its application to healthy and ischemia-reperfusion rats pharmacokinetic studies.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:37952449] [10.1016/j.jpba.2023.115852]

3. Xu Rui-Qi, Ma Ling, Chen Timson, Zhang Wei-Xiong, Chang Kuan, Wang Jing.  (2023)  Sophorolipid inhibits histamine-induced itch by decreasing PLC/IP3R signaling pathway activation and modulating TRPV1 activity.  Scientific Reports,  13  (1): (1-13).  [PMID:37198299] [10.1038/s41598-023-35158-9]

4. Huang Wenwen, Zhou Xiaoying.  (2022)  Anti-histamine effects of dipotassium glycyrrhizinate on lung fibroblasts, implicating its therapeutic mechanism for pulmonary fibrosis.  JOURNAL OF PHARMACY AND PHARMACOLOGY,  74  (9): (1241-1250).  [PMID:35788858] [10.1093/jpp/rgac030]

5. Xian-Mei Song, Bing-Jie Li, Yan-Yan Zhang, Wen-Jing Ge, She-Feng Zhang, Wei-Feng Cui, Geng-Sheng Li, Rui-Feng Liang.  (2021)  Rutaecarpine enhances the anti-diabetic activity and hepatic distribution of metformin via up-regulation of Oct1 in diabetic rats.  XENOBIOTICA,      [PMID:33952086] [10.1080/00498254.2021.1926573]

6. Jadera Talap, Zhuowei Shen, Jing Nie, Jie Pan, Mingcheng Xu, Kui Zeng, Kaifeng He, Fengting Ou, Houhong He, Jianbiao Yao, Ruwei Wang, Lushan Yu, Su Zeng.  (2021)  The characterisation of the in vitro metabolism and transport of 6-hydroxykynurenic acid, an important constituent of Ginkgo biloba extracts.  XENOBIOTICA,      [PMID:33512253] [10.1080/00498254.2021.1881654]

7. Chen Jiangfei, Guo Suhang, Yu Xianzhu, Lei Jinxiu, Xu Tao, Zhu Suyan, Chen Lu, Xu Ping, Zhou Xuan, Yu Lushan.  (2020)  Metabolic interactions between flumatinib and the CYP3A4 inhibitors erythromycin, cyclosporine, and voriconazole.  PHARMAZIE,  75  (9): (424-429).  [PMID:32797767] [10.1691/ph.2020.0068]

8. Peng Wei, Han Ping, Yu Luyao, Chen Ying, Ye Bingzhu, Qin Luping, Xin Hailiang, Han Ting.  (2019)  Anti-allergic rhinitis effects of caffeoylquinic acids from the fruits of Xanthium strumarium in rodent animals via alleviating allergic and inflammatory reactions.  Revista Brasileira de Farmacognosia-Brazilian Journal of Pharmacognosy,  29  (1): (46-53).  [PMID:] [10.1016/j.bjp.2018.10.004]

9. Xiu Chen, Xiaoyi Pan, Jieping Zhao, Huihui Jin, Hengbin Zhang, Yongbiao Song, Hui Zhou, Jianbiao Yao, Huidi Jiang.  (2025)  Interactions of neocryptotanshinone and human cytochrome P450 in silico and in vitro.  TOXICOLOGY IN VITRO,      [PMID:41419033] [10.1016/j.tiv.2025.106191]

10. Xiaoying Wu, Zhanzhe Ge, Haojie Zhan, Mengxiang Zheng, Yiming Feng, Yajun Zhai, Li Yuan, Jianhua Liu, Yushan Pan, Gongzheng Hu, Xiaoyuan Ma, Dandan He.  (2026)  Repurposing loratadine to reverse colistin resistance in Klebsiella pneumoniae through targeting lipid A modification.  Emerging Microbes & Infections,      [PMID:41678146] [10.1080/22221751.2026.2623697]