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Technical Data
| Formula | C22H23ClN2O2 |
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| Molecular Weight | 382.88 | CAS No. | 79794-75-5 | ||||
| Solubility (25°C)* | In vitro | Ethanol | 77 mg/mL (201.1 mM) | ||||
| DMSO | 17 mg/mL (44.4 mM) | ||||||
| Water | Insoluble | ||||||
| In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Loratadine 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. | ||||
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| 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. [1] 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. [2] 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). [3] 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. [4] 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. [5] |
Protocol (from reference)
References
Selleck's Loratadine has been cited by 10 publications
| Mast cell activation triggered by SARS-CoV-2 causes inflammation in brain microvascular endothelial cells and microglia [ Front Cell Infect Microbiol, 2024, 14:1358873] | PubMed: 38638822 |
| Mast cell activation triggered by SARS-CoV-2 causes inflammation in brain microvascular endothelial cells and microglia [ Front Cell Infect Microbiol, 2024, 14:1358873] | PubMed: 38638822 |
| Immuno-oncological effects of standard anticancer agents and commonly used concomitant drugs: an in vitro assessment [ BMC Pharmacol Toxicol, 2024, 25(1):25] | PubMed: 38444002 |
| Immuno-oncological effects of standard anticancer agents and commonly used concomitant drugs: an in vitro assessment [ BMC Pharmacol Toxicol, 2024, 25(1):25] | PubMed: 38444002 |
| Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] | PubMed: 35868306 |
| Combinational benefit of antihistamines and remdesivir for reducing SARS-CoV-2 replication and alleviating inflammation-induced lung injury in mice [ Zool Res, 2022, 43(3):457-468] | PubMed: 35503561 |
| Histamine signaling and metabolism identify potential biomarkers and therapies for lymphangioleiomyomatosis [ EMBO Mol Med, 2021, e13929] | PubMed: 34378323 |
| Project IDentif.AI: Harnessing Artificial Intelligence to Rapidly Optimize Combination Therapy Development for Infectious Disease Intervention [ Adv Ther (Weinh), 2020, 2000034] | PubMed: 32838027 |
| Quantifying Drug Combination Synergy along Potency and Efficacy Axes. [ Cell Syst, 2019, 8(2):97-108] | PubMed: 30797775 |
| Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms. [ Anticancer Res, 2019, 39(7):3767-3775] | PubMed: 31262903 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.