Loratadine (Synonyms: 氯雷他定; Loratidine; SCH 29851)

目录号: HY-17043 纯度: 99.98%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Loratadine (SCH-29851) 是 histamine H1 受体反向激动剂，IC50>32 μM。Loratadine 具有抗登革热病毒 (DENV) 的活性。Loratadine 能抑制炎症介质的免疫释放。

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Loratadine Chemical Structure

CAS No. : 79794-75-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥176	In-stock
50 mg	￥160	In-stock
100 mg	￥200	In-stock
500 mg	￥500	In-stock
1 g		询价
5 g		询价

or 大包装询价

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Other Forms of Loratadine:

MCE 顾客使用本产品发表的 6 篇科研文献

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

生物活性
纯度 & 产品资料
参考文献

生物活性

Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

IC₅₀ & Target

H₁ Receptor

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	15.13 μM Compound: LORATADINE	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
Caco-2	CC₅₀	28.33 μM Compound: LORATADINE	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
CHO	IC₅₀	11.4 μM Compound: loratadine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	4 μM Compound: 1	Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay	[PMID: 25318072]
HEK293	IC₅₀	63.4 μM Compound: 24	Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay	[PMID: 31260312]
HepG2	EC₅₀	10 μM Compound: Loratadine	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	12.6 μM Compound: Loratadine	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	3 μM Compound: 8	Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay	[PMID: 23688559]
HT-29	IC₅₀	6.2 μM Compound: Loratadine	Cytotoxicity against human HT-29 cells after 72 hrs by crystal violet staining Cytotoxicity against human HT-29 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
HT-29	IC₅₀	6.2 μM Compound: 4	Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
MCF7	IC₅₀	7.5 μM Compound: Loratadine	Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
MCF7	IC₅₀	7.5 μM Compound: 4	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
MDA-MB-231	IC₅₀	8.4 μM Compound: Loratadine	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by crystal violet staining Cytotoxicity against human MDA-MB-231 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
MDA-MB-231	IC₅₀	8.4 μM Compound: 4	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]

体外研究
(In Vitro)

Loratadine is an antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

382.88

Formula

C₂₂H₂₃ClN₂O₂

CAS 号

79794-75-5

性状

固体

颜色

White to off-white

中文名称

氯雷他定；氯羟他定；诺那他定；氯雷他啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (130.59 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.53 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.53 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.53 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98%

选择批次：

Data Sheet (631 KB) SDS (458 KB)

COA (293 KB) HNMR (129 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Kay GG, Harris AG. Loratadine: a non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin Exp Allergy. 1999 Jul;29 Suppl 3:147-50. [Content Brief]

[2]. Menardo JL, Horak F, Danzig MR, Czarlewski W. A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4. [Content Brief]

[3]. Monroe EW. Loratadine in the treatment of urticaria. Clin Ther. 1997 Mar-Apr;19(2):232-42. [Content Brief]

[4]. Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs. 1994 Oct;48(4):617-37. [Content Brief]

[5]. Roman IJ, Danzig MR. Loratadine. A review of recent findings in pharmacology, pharmacokinetics, efficacy, and safety, with a look at its use in combination with pseudoephedrine. Clin Rev Allergy. 1993 Spring;11(1):89-110. [Content Brief]

[6]. Shahen M, et al. Dengue virus causes changes of MicroRNA-genes regulatory network revealing potential targets for antiviral drugs. BMC Syst Biol. 2018 Jan 4;12(1):2. [Content Brief]

[7]. Kleine-Tebbe J, et al. Inhibition of IgE- and non-IgE-mediated histamine release from human basophil leukocytes in vitro by a histamine H1-antagonist, desethoxycarbonyl-loratadine. J Allergy Clin Immunol. 1994;93(2):494-500. [Content Brief]

Loratadine 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6118 mL	13.0589 mL	26.1178 mL	65.2946 mL
	5 mM	0.5224 mL	2.6118 mL	5.2236 mL	13.0589 mL
	10 mM	0.2612 mL	1.3059 mL	2.6118 mL	6.5295 mL
	15 mM	0.1741 mL	0.8706 mL	1.7412 mL	4.3530 mL
	20 mM	0.1306 mL	0.6529 mL	1.3059 mL	3.2647 mL
	25 mM	0.1045 mL	0.5224 mL	1.0447 mL	2.6118 mL
	30 mM	0.0871 mL	0.4353 mL	0.8706 mL	2.1765 mL
	40 mM	0.0653 mL	0.3265 mL	0.6529 mL	1.6324 mL
	50 mM	0.0522 mL	0.2612 mL	0.5224 mL	1.3059 mL
	60 mM	0.0435 mL	0.2176 mL	0.4353 mL	1.0882 mL
	80 mM	0.0326 mL	0.1632 mL	0.3265 mL	0.8162 mL
	100 mM	0.0261 mL	0.1306 mL	0.2612 mL	0.6529 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Loratadine79794-75-5Loratidine SCH 29851氯雷他定氯羟他定诺那他定氯雷他啶SCH29851SCH 29851SCH-29851Dengue virusFlavivirusHistamine ReceptorDENVInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Loratadine (Synonyms: 氯雷他定; Loratidine; SCH 29851)

Customer Review

Other Forms of Loratadine:

MCE 顾客使用本产品发表的 6 篇科研文献