Lersivirine

Name: Lersivirine
Brand: TargetMol
SKU: T7700
Price: 143 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 98.01%

货号 T7700Cas号 473921-12-9

别名 UK-453061, Lersivirine(UK 453061), 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈

Lersivirine (UK-453061) 是非核苷逆转录的抑制剂 (NNRTI)，有效抑制 NNRTI 耐药病毒。它对野生型人类免疫缺陷病毒和临床相关 NNRTI 耐药菌株显示出强大的抗逆转录病毒活性。

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Lersivirine

一键复制产品信息

很棒

纯度: 98.01%

货号 T7700 别名 UK-453061, Lersivirine(UK 453061), 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈Cas号 473921-12-9

规格	价格	库存
1 mg	¥ 143	现货
5 mg	¥ 342	现货
10 mg	¥ 541	现货
25 mg	¥ 1,070	现货
50 mg	¥ 1,620	现货
100 mg	¥ 2,310	现货
200 mg	¥ 3,230	现货
1 mL x 10 mM (in DMSO)	¥ 376	现货

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产品介绍

Lersivirine AI Summary

Lersivirine exhibits significant antiviral activity against HIV with IC50 values of 4.0 nM and 119.0 nM in different assays. It targets multiple HIV reverse transcriptase mutants with IC95 values ranging from 40.0 nM to 100.0 nM and shows an ability to inhibit both non-competitively and competitively. The compound has low cytotoxicity toward human cells with CC30 values above 30.0 µM, and CC50 values greater than 100,000 nM in certain assays, indicating a high selectivity index. It maintains metabolic stability with a half-life of 1.217 hours in human liver microsomes and demonstrates a half-life of approximately 6.223 hours in healthy human plasma. Pharmacokinetic data shows a peak plasma concentration (Cmax) of about 4910.43 nM and an area under the curve (AUC) of 10967.32 ng.hr.mL-1. Additionally, coadministration with an antacid affects its Tmax, which is 5.0 hours compared to 2.0 hours when administered alone. Moreover, Lersivirine exhibits activity against other viral infections, including SARS-CoV-2, showing cytotoxicity inhibition in Caco-2 and VERO-6 cells at a concentration of 10 µM. It also shows inhibition percentages against SARS-CoV-2 3CL-Pro protease at 20 µM. The compound demonstrates inhibitory activity against the human HDAC6 enzyme and induces the activity of CYP3A, influencing midazolam metabolism. In addition to its antiviral properties, Lersivirine shows antitrypanocidal activity against Trypanosoma brucei and antileishmanial and antiplasmodial activities, albeit with IC50 values indicating low potency in these assays. Overall, Lersivirine presents a broad spectrum of bioactivities with notable efficacy against HIV and potential applications against other viral infections and parasitic diseases..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.
靶点活性	NNRT:119 nM (IC50)
别名	UK-453061, Lersivirine(UK 453061), 3-氰基-5-[[3,5-二乙基-1-(2-羟基乙基)-1H-吡唑-4-基]氧基]苯腈

化学信息

分子量	310.35
分子式	C₁₇H₁₈N₄O₂
CAS No.	473921-12-9
Smiles	CCc1nn(CCO)c(CC)c1Oc1cc(cc(c1)C#N)C#N
密度	1.19

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 50 mg/mL (161.11 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (8.06 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	3.2222 mL	16.1108 mL	32.2217 mL	161.1084 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL	32.2217 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 mL	16.1108 mL
20 mM	0.1611 mL	0.8055 mL	1.6111 mL	8.0554 mL
50 mM	0.0644 mL	0.3222 mL	0.6444 mL	3.2222 mL
100 mM	0.0322 mL	0.1611 mL	0.3222 mL	1.6111 mL