473921-12-9|勒西韦林|Lersivirine|MFCD16619314-范德生物科技公司

勒西韦林

NMR下载 COA and HPLC MSDS下载
names：
Lersivirine
CAS号：
473921-12-9
MDL Number： MFCD16619314
MF(分子式)： C17H18N4O2 MW(分子量)： 310.35
EINECS:No data available Reaxys Number:No data available
Pubchem ID:16739244 Brand:BIOFOUNT

勒西韦林(Lersivirine,473921-12-9,UK-453061)是正在开发中的用于治疗HIV-1感染的下一代非核苷类逆转录酶抑制剂（NNRTI）。 UK-453061可以防止HIV进入健康的CD4细胞核，从而阻止细胞产生新病毒并减少体内病毒的数量。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM000649-10mg	10mg	98.01%	¥ 1883.00	¥ 1883.00		2-3天	- +	¥ 0.00
YZM000649-5mg	5mg	98.01%	¥ 1088.10	¥ 1088.10		2-3天	- +	¥ 0.00

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中文别名	勒西韦林(473921-12-9);
英文别名	Lersivirine(473921-12-9);lersivirine;UK 453,061;UK 453061;UK-453,061;UK-453061;UK453,061;UK453061;5-((3,5-diethyl-1-(2-hydroxyethyl)(3,5-14C2)-1H-pyrazol-4-yl)oxy)benzene-1,3-dicarbonitrile;
CAS号	473921-12-9
SMILES	CCC1=NN(CCO)C(CC)=C1OC2=CC(C#N)=CC(C#N)=C2
Inchi	InChI = 1S / C17H18N4O2 / c1-3-15-17（16（4-2）21（20-15）5-6-22）23-14-8-12（10-18）7-13（9- 14）11-19 / h7-9,22H，3-6H2,1-2H3
InchiKey	MCPUZZJBAHRIPO-UHFFFAOYSA-N
分子式 Formula	C17H18N4O2
分子量 Molecular Weight	310.35
闪点 FP	229.2±28.7°摄氏度
熔点 Melting point	No data available
沸点 Boiling point	760毫米汞柱时为455.4±45.0°C
Polarizability极化度	No data available
密度 Density	1.2±0.1克/厘米3
蒸汽压 Vapor Pressure	25°C时0.0±1.2 mmHg
溶解度Solubility	生物体外In Vitro:DMSO溶解度50 mg/mL(161.11 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble)
性状	固体粉末,Power
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

勒西韦林(Lersivirine,473921-12-9,UK-453061)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags：UK-453061试剂,UK-453061杂质,UK-453061中间体,UK-453061合成,UK-453061密度,UK-453061闪点,UK-453061溶解度,UK-453061旋光度,UK-453061购买,UK-453061MSDS,

产品说明	勒西韦林(Lersivirine,473921-12-9,UK-453061)是逆转录酶抑制剂,UK-453061是抗HIV剂.
Introduction	勒西韦林(Lersivirine,473921-12-9,UK-453061)is a reverse transcriptase inhibitor, UK-453061 is an anti-HIV agent.
Application1	Lersivirine（UK-453061）是新一代非核苷类逆转录酶抑制剂（NNRTI，IC50 = 119 nM），具有独特的耐药性，对野生型人免疫缺陷病毒和临床相关的NNRTI耐药株表现出有效的抗逆转录病毒活性。
Application2	Lersivirine（UK-453061）是非核苷逆转录酶抑制剂（NNRTI），IC50为119 nM，对野生型和NNRTI抗性型毒株都有效。
Application3

勒西韦林(Lersivirine,473921-12-9,UK-453061)药理学：

※Lersivirine是下一代吡唑非核苷逆转录酶抑制剂。Lersivirine保留抗HIV病毒在位置Y181突变，这在赋予抗性活性依非韦伦，依曲韦林和奈韦拉平。

※Lersivirine是正在开发中的用于治疗HIV-1感染的下一代非核苷类逆转录酶抑制剂（NNRTI）。它可以防止HIV进入健康的CD4细胞核，从而阻止细胞产生新病毒并减少体内病毒的数量。

※Lersivirine（UK-453061）是新一代非核苷类逆转录酶抑制剂（NNRTI，IC50 = 119 nM），具有独特的耐药性，对野生型人免疫缺陷病毒和临床相关的NNRTI耐药株表现出有效的抗逆转录病毒活性。； IC50值：0.119 uM [1]；目标：

※NNRTIUK-453061（化合物5）显示出对大批野生型和耐药HIV的优异活性，与针对分离的RT酶的令人鼓舞的特性一致。借助于有效和简洁的合成途径，可以容??易地以克数制备化合物5。该化合物还具有良好的水溶性和配制特性，

※Lersivirine（UK-453061）是非核苷逆转录酶抑制剂（NNRTI），IC50为119 nM，对野生型和NNRTI抗性型毒株都有效。

※Lersivirine（UK-453061）是新一代非核苷类逆转录酶抑制剂（NNRTI，IC50 = 119 nM），具有独特的耐药性，对野生型人免疫缺陷病毒和临床相关的NNRTI耐药株表现出有效的抗逆转录病毒活性。IC50值：0.119 uM ,目标：NNRTI UK-453061（化合物5）显示出对大批野生型和耐药HIV的优异活性，与针对分离的RT酶的令人鼓舞的特性一致。借助于有效和简洁的合成途径，可以容易地以克数制备化合物5。该化合物还具有良好的水溶性和配制特性，可进一步进行体内评估。评估5（UK-453,061，lersivirine）治疗HIV感染潜力的临床试验正在进行中，并将在适当的时候报告进一步的进展。在临床相关的lersivirine剂量（每日总剂量500-1,000 mg）下，咪达唑仑的平均血浆暴露以剂量依赖性方式降低20-36％。莱西韦林1,000 mg QD与OC的共同给药对PK的影响较小，乙炔雌二醇暴露量增加10％，左炔诺孕酮暴露量减少13％[2]。交配的Crl：CD1（ICR）小鼠在妊娠第6至17天每天口服一次给予0、150、350和500 mg / kg lersivirine，然后在妊娠第18天进行剖宫产。大剂量组以250 mg / kg的剂量进行，以诱导肝代谢酶.

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

勒西韦林(Lersivirine,473921-12-9,UK-453061)危害标识：

象形图
信号	Warning
GHS危险说明	Aggregated GHS information provided by 29 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
	H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]
	H373 (100%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]
	H412 (100%): Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]
	Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码	P201, P202, P260, P273, P281, P308+P313, P314, P405, and P501
防范说明代码	(The corresponding statement to each P-code can be found at the GHS Classification page.)

Mowbray CE, et al. Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5857-60.

Davis J, et al. The effect of lersivirine, a next-generation NNRTI, on the pharmacokinetics of midazolam and oral contraceptives in healthy subjects. Eur J Clin Pharmacol. 2012 Nov;68(11):1567-72.

Cappon GD, et al. Developmental toxicity study of lersivirine in mice. Birth Defects Res B Dev Reprod Toxicol. 2012 Jun;95(3):225-30.

The effect of lersivirine, a next-generation NNRTI, on the pharmacokinetics of midazolam and oral contraceptives in healthy subjects European Journal of Clinical Pharmacology 2012 22527351

No effect of a single supratherapeutic dose of lersivirine, a next-generation NNRTI, on QTc interval in healthy subjects Journal of the International AIDS Society 2010

勒西韦林(Lersivirine,473921-12-9,UK-453061)参考文献:

1.Mild palladium-catalyzed cyanation of (hetero)aryl halides and triflates in aqueous media.
Cohen DT1, Buchwald SL. Org Lett. 2015 Jan 16;17(2):202-5. doi: 10.1021/ol5032359. Epub 2015 Jan 2.

A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.

2.Two-year carcinogenicity study in rats with a nonnucleoside reverse transcriptase inhibitor.
Nambiar PR1, Morton D2, Dochterman LW3, Houle C4, Thomford PJ3, Fate G4, Bailey SA5, Finch GL4. Toxicol Pathol. 2015 Apr;43(3):354-65. doi: 10.1177/0192623314544381. Epub 2014 Aug 13.

Administration of lersivirine, a nonnucleotide reverse transcriptase inhibitor, daily by oral gavage to Sprague-Dawley rats for up to 2 yr was associated with decreased survival, decreased body weights, and an increase in neoplasms and related proliferative lesions in the liver, thyroid, kidney, and urinary bladder. Thyroid follicular adenoma and carcinoma, the associated thyroid follicular hypertrophy/hyperplasia, hepatocellular adenoma/adenocarcinoma, altered cell foci, and hepatocellular hypertrophy were consistent with lersivirine-related induction of hepatic microsomal enzymes. Renal tubular adenoma and renal tubular hyperplasia were attributed to the lersivirine-related exacerbation of chronic progressive nephropathy (CPN), while urinary bladder hyperplasia and transitional cell carcinoma in the renal pelvis and urinary bladder were attributed to urinary calculi. Renal tubular neoplasms associated with increased incidence and severity of CPN, neoplasms of transitional epithelium attributed to crystalluria, and thyroid follicular and hepatocellular neoplasms related to hepatic enzyme induction have low relevance for human risk assessment.

3.The HIV-1 non-nucleoside reverse transcriptase inhibitors (part V): capravirine and its analogues.
Li X1, Zhan P, De Clercq E, Liu X. Curr Med Chem. 2012;19(36):6138-49.

Capravirine (S-1153, AG1549), a 1,2,4,5-tetrasubstituted imidazole derivative, was firstly reported by the Shionogi company to inhibit HIV-1 strains which were resistant to other NNRTIs. However, safety and efficacy studies showed that capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb. Notwithstanding, with aim to obtain novel inhibitors against drug-resistant HIV-1 strains, an in-depth analysis of the particular binding mode of capravirine, together with the wide use of analogue-based chemical evolution strategies, such as bioisosteric replacement, molecular hybridization, prodrug approach, ligand efficiency, etc., gave a huge impetus to the optimization of capravirine. Especially, lersivirine (UK-453,061) was selected for further clinical evaluation due to its very impressive potency against a broad panel of key HIV-1 mutants, safety, pharmacokinetics and other pharmaceutical factors.

4.Efficacy and safety of lersivirine (UK-453,061) versus efavirenz in antiretroviral treatment-naive HIV-1-infected patients: week 48 primary analysis results from an ongoing, multicenter, randomized, double-blind, phase IIb trial.
Vernazza P1, Wang C, Pozniak A, Weil E, Pulik P, Cooper DA, Kaplan R, Lazzarin A, Valdez H, Goodrich J, Mori J, Craig C, Tawadrous M. J Acquir Immune Defic Syndr. 2013 Feb 1;62(2):171-9. doi: 10.1097/QAI.0b013e31827a2ba2.

OBJECTIVE: A 96-week clinical study was planned to estimate the antiviral activity and safety of lersivirine in treatment-naive HIV-1-infected patients.

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