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Lofepramine

Name: Lofepramine
Brand: TargetMol
SKU: T15773
Price: 296 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.38%

货号 T15773Cas号 23047-25-8

别名 洛非帕明, Lopramine, Leo 640, Gamanil, Amplit

Lofepramine (Leo 640) 是一种有效的三环抗抑郁药，广泛地代谢为 Desipramine。它能够抑制摄取促进去甲肾上腺素能神经传递，以及抑制神经元摄取 5-羟色胺和色氨酸吡咯酶，增强 5-羟色胺能神经传递，进而发挥其抗抑郁作用。它还具有显著的抗焦虑效果。

为众多的药物研发团队赋能，

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Lofepramine

一键复制产品信息

很棒

纯度: 98.38%

货号 T15773 别名 洛非帕明, Lopramine, Leo 640, Gamanil, AmplitCas号 23047-25-8

规格	价格	库存
1 mg	¥ 296	现货
5 mg	¥ 662	现货
10 mg	¥ 892	现货
25 mg	¥ 1,720	现货
50 mg	¥ 2,580	现货
100 mg	¥ 3,870	现货
200 mg	¥ 5,530	现货
1 mL x 10 mM (in DMSO)	¥ 597	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

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纯度: 98.38%

颜色: 黄色

性状: Solid

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资源下载:

COA HPLC HNMR 产品操作手册

产品介绍

Lofepramine AI Summary

Lofepramine exhibits diverse bioactivity profiles and some degree of pharmacokinetic complexity. It has a high partition coefficient (LogD = 4.58) and a slightly acidic pKa of 6.7, indicating possible pH-dependent solubility changes with a delta logD of -0.32 from pH 6.5 to 7.4. Despite these characteristics, its oral bioavailability in humans is low, with F ≤ 20.0%. This compound functions as an inhibitor across multiple biological targets. It inhibits acid sphingomyelinase (ASM) in human H4 cells (90.5% residual activity at 10 μM), Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 44668.4 nM, and Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) with potencies ranging from 15848.9 nM to 50118.7 nM. It also inhibits Histone Lysine Methyltransferase G9a (1258.9 nM), the vitamin D receptor (VDR) (35481.3-39810.7 nM), delayed death in malarial parasite plastid (12589.3-15101.4 nM), USP1/UAF1 (35481.3 nM), and induces DNA re-replication in various cell lines (33498.3 nM). However, it shows weak inhibitory activity in kinase assays against GST-RET proteins (IC50 > 20000.0 nM), and low potency in blocking uptake of substrates in human BSEP, MRP2, MRP3, and MRP4 transport proteins (IC50 > 133000.0 nM). In terms of antimicrobial activity, Lofepramine does not show significant effectiveness against Candida albicans, Cryptococcus neoformans, and various bacteria including Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus MRSA (MIC > 10000.0 nM). It also exhibits a high CC50 value for cytotoxicity against HEK293 cells (CC50 > 10000.0 nM). Despite moderate activity in certain viability assays against SARS-CoV-2-infected Vero E6 cells (inhibition index = 0.7416), it shows antiviral activity manifested by a 17.72% inhibition of SARS-CoV-2 cytotoxicity in Caco-2 cells at 10 μM after 48 hours and 64.61% inhibition of SARS-CoV-2 3CL-Pro protease at 20 μM. The IC50 value for VERO-6 cell cytotoxicity inhibition is greater than 20000.0 nM, indicating moderate to low potency. Lofepramine's activity includes 35.11% inhibition of human HDAC6 with a commercial substrate and 0.27% with a custom substrate, alongside various binding affinities and activities towards SLC6A2, SLC6A4, HRH1, DRD2, OPRK1, CHRM2, CNR1, NR1I2, HRH2, Ptgs1, and PDE4D. Liver toxicity has been associated with Lofepramine, including moderate hepatotoxicity (46.5% of cases), and acute liver toxicity characterized by cytolytic and choleostatic effects, though severe chronic liver diseases and secondary liver conditions are not significantly linked. Overall, Lofepramine shows potential as a multi-target inhibitor, with notable activity in certain pathways and processes, yet limited oral bioavailability and specific safety concerns necessitate cautious therapeutic consideration..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Lofepramine (Leo 640) is a potent tricyclic antidepressant that is extensively metabolized to desipramine. It inhibits the serotonin and norepinephrine transporters by inhibiting neurons with Kd values of 70 and 5.4 nM, respectively, with weak antagonism of serotonin, histamine and muscarinic receptors.
靶点活性	5-HT:70 nM(Kd), NET:5.4 nM(Kd)
别名	洛非帕明, Lopramine, Leo 640, Gamanil, Amplit

化学信息

分子量	418.96
分子式	C₂₆H₂₇ClN₂O
CAS No.	23047-25-8
Smiles	C(CCN(CC(=O)C1=CC=C(Cl)C=C1)C)N2C=3C(CCC=4C2=CC=CC4)=CC=CC3
密度	1.173g/cm3

储存&溶解度

存储

溶解度信息

DMSO: 48 mg/mL (114.57 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 2 mg/mL (4.77 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3869 mL	11.9343 mL	23.8686 mL	119.3431 mL
5 mM	0.4774 mL	2.3869 mL	4.7737 mL	23.8686 mL
10 mM	0.2387 mL	1.1934 mL	2.3869 mL	11.9343 mL
20 mM	0.1193 mL	0.5967 mL	1.1934 mL	5.9672 mL
50 mM	0.0477 mL	0.2387 mL	0.4774 mL	2.3869 mL
100 mM	0.0239 mL	0.1193 mL	0.2387 mL	1.1934 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法： 取 100 μL DMSO 母液，添加 400 μL PEG300 混匀澄清，再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH₂O 混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300， PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多

关键词

serotonin reuptake norepinephrine reuptake Lofepramine Inhibitor inhibit 5HTReceptor 5HT Receptor

Lofepramine

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产品介绍

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体内实验配液计算器

剂量转换

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