Loratadine (Synonyms: SCH 29851) |
Catalog No.GC15252
One-Click Copy Product Info
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Loratadine is a non- sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H 1 receptors (K i = 35 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 79794-75-5
Sample solution is provided at 25 µL, 10mM.
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Loratadine is a non- sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H 1 receptors (K i = 35 nM). It is a second-generation antihistamine that is often used to treat allergy symptoms. It can inhibit immunologic release of inflammatory mediators[1-3].
Loratadine(75 µM loratadine;24 hours) pre-treatment of exponentially growing cells increased radiation-induced cytotoxicity[4]. Loratadine (10 µM) inhibited TRPV2-dependent responses in a primary culture of mouse endometrial stromal cells and attenuated cell proliferation and migration in cell proliferation and wound healing assays[5]. The expression of H1R was dose-responsively induced by Advanced glycation end products (AGEs) in chondrocytes. Treatment with loratadine((25/50 µM; 24 h) mitigated AGEs-induced oxidative stress, as revealed by suppressed production of mitochondrial ROS and the NADPH oxidase subunit NOX4[6].
Loratadine(5,10 mg/kg; p.o.) significantly reduced gastric bleeding in mice. Loratadine suppress inflammation by specifically targeting TAK1 and suppressing consequent AP-1 signaling pathway activation and inflammatory cytokine production[7]. In ICR mice, single oral administration of loratadine at a dose of 5 or 10 mg/kg significantly inhibited the dorsal scratching behavior induced by histamine or an antigen[8].
References:
[1]. AlMasoud N, Bakheit AH, et,al. Loratadine. Profiles Drug Subst Excip Relat Methodol. 2022;47:55-90. doi: 10.1016/bs.podrm.2021.10.002. Epub 2021 Dec 7. PMID: 35396016.
[2]. Kreutner W, Chapman RW, et,al. Antiallergic activity of loratadine, a non-sedating antihistamine. Allergy. 1987 Jan;42(1):57-63. doi: 10.1111/j.1398-9995.1987.tb02188.x. PMID: 2436504.
[3]. Hunto ST, Kim HG, et,al. Loratadine, an antihistamine drug, exhibits anti-inflammatory activity through suppression of the NF-kB pathway. Biochem Pharmacol. 2020 Jul;177:113949. doi: 10.1016/j.bcp.2020.113949. Epub 2020 Apr 3. PMID: 32251678.
[4]. Soule BP, Simone NL, et,al. Loratadine dysregulates cell cycle progression and enhances the effect of radiation in human tumor cell lines. Radiat Oncol. 2010 Feb 3;5:8. doi: 10.1186/1748-717X-5-8. PMID: 20128919; PMCID: PMC2829588.
[5]. Van den Eynde C, Held K, et,al. Loratadine, an antihistaminic drug, suppresses the proliferation of endometrial stromal cells by inhibition of TRPV2. Eur J Pharmacol. 2022 Aug 5;928:175086. doi: 10.1016/j.ejphar.2022.175086. Epub 2022 Jun 14. PMID: 35714693.
[6]. Gao F, Zhang S. Loratadine Alleviates Advanced Glycation End Product-Induced Activation of NLRP3 Inflammasome in Human Chondrocytes. Drug Des Devel Ther. 2020 Jul 21;14:2899-2908. doi: 10.2147/DDDT.S243512. PMID: 32801633; PMCID: PMC7382759.
[7].Jang J, Hunto ST, et,al. Anti-Inflammatory Activities of an Anti-Histamine Drug, Loratadine, by Suppressing TAK1 in AP-1 Pathway. Int J Mol Sci. 2022 Apr 3;23(7):3986. doi: 10.3390/ijms23073986. PMID: 35409346; PMCID: PMC8999734.
[8]. Hossen MA, Fujii Y, et,al. Effect of loratadine on mouse models of atopic dermatitis associated pruritus. Int Immunopharmacol. 2005 Jul;5(7-8):1331-6. doi: 10.1016/j.intimp.2005.02.004. Epub 2005 Mar 9. PMID: 15914337.
| Cell experiment [1]: | |
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Cell lines |
HT29 cells |
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Preparation Method |
Cells were treated with loratadine. Then, cells were treated with varying doses of radiation using an Eldorado 8 cobalt-60 teletherapy unit. |
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Reaction Conditions |
75 µM loratadine;24 hours |
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Applications |
Loratadine pre-treatment of exponentially growing cells increased radiation-induced cytotoxicity. |
| Animal experiment [2]: | |
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Animal models |
ICR mice (Acute Gastritis Induction) |
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Preparation Method |
Loratadine-treated groups were orally injected with 5 mg/kg or 10 mg/kg Loratadine solution. |
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Dosage form |
5,10 mg/kg; p.o. |
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Applications |
Loratadine significantly reduced gastric bleeding. |
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References: [1]. Soule BP, Simone NL, et,al. Loratadine dysregulates cell cycle progression and enhances the effect of radiation in human tumor cell lines. Radiat Oncol. 2010 Feb 3;5:8. doi: 10.1186/1748-717X-5-8. PMID: 20128919; PMCID: PMC2829588. |
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| Cas No. | 79794-75-5 | SDF | |
| Synonyms | SCH 29851 | ||
| Chemical Name | ethyl 4-(8-chloro-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridin-11-ylidene)piperidine-1-carboxylate | ||
| Canonical SMILES | CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1 | ||
| Formula | C22H23ClN2O2 | M.Wt | 382.88 |
| Solubility | ≥ 19.144mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6118 mL | 13.0589 mL | 26.1178 mL |
| 5 mM | 522.4 μL | 2.6118 mL | 5.2236 mL |
| 10 mM | 261.2 μL | 1.3059 mL | 2.6118 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)