Loratadine
(Synonyms: 氯雷他定; Loratidine; SCH 29851) 目录号 : GC15252
Loratadine is a non- sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H 1 receptors (K i = 35 nM).
Cas No.:79794-75-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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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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].
氯雷他定Loratadine是一种非镇静性抗组胺药,作用于选择性的外周组胺H1受体的反向激动剂(Ki=35 nM)。它是第二代抗组胺药,常用于治疗过敏症状。它可以抑制免疫学释放炎症介质[1-3]。
Loratadine(75 µM loratadine;24 hours)对指数生长的细胞进行预处理可增加辐射引起的细胞毒性[4]。Loratadine (10 µM) 可以抑制小鼠子宫内膜基质细胞的TRPV2依赖性反应,并在细胞增殖和伤口愈合试验中减弱细胞增殖和迁移[5]。晚期糖基化终产物(AGEs)可以剂量依赖性诱导软骨细胞中H1R表达。Loratadine (25/50 µM；24 h)的处理可以缓解AGEs诱导的氧化应激,表现为抑制线粒体ROS和NADPH氧化酶亚基NOX4的产生[6]。
Loratadine(5,10 mg/kg; p.o.)可以显著减少小鼠的胃出血。Loratadine通过特异性靶向TAK1并抑制随后的AP-1信号通路激活和炎症细胞因子的产生来抑制炎症[7]。在ICR小鼠中,单次口服5或10 mg/kg的Loratadine可以显著抑制组胺或抗原诱导的背部抓痒行为[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.
| Cas No. | 79794-75-5 | SDF | |
| 别名 | 氯雷他定; Loratidine; SCH 29851 | ||
| 化学名 | 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 | ||
| 分子式 | C22H23ClN2O2 | 分子量 | 382.88 |
| 溶解度 | ≥ 19.144mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6118 mL | 13.0589 mL | 26.1178 mL |
| 5 mM | 0.5224 mL | 2.6118 mL | 5.2236 mL |
| 10 mM | 0.2612 mL | 1.3059 mL | 2.6118 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。