購(gòu)物車(chē) 
-
勒西韋林
- names：
Lersivirine
- CAS號(hào)：
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
勒西韋林(Lersivirine,473921-12-9,UK-453061)是正在開(kāi)發(fā)中的用于治療HIV-1感染的下一代非核苷類(lèi)逆轉(zhuǎn)錄酶抑制劑（NNRTI）。 UK-453061可以防止HIV進(jìn)入健康的CD4細(xì)胞核，從而阻止細(xì)胞產(chǎn)生新病毒并減少體內(nèi)病毒的數(shù)量。
| 貨品編碼 | 規(guī)格 | 純度 | 價(jià)格 (￥) | 現(xiàn)價(jià)(￥) | 特價(jià)(￥) | 庫(kù)存描述 | 數(shù)量 | 總計(jì) (￥) |
|---|---|---|---|---|---|---|---|---|
| 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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| 中文別名 | 勒西韋林(473921-12-9); |
| 英文別名 | 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號(hào) | 473921-12-9 |
| 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 |
| 溶解度Solubility | 生物體外In Vitro:DMSO溶解度50 mg/mL(161.11 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble) |
| 性狀 | 固體粉末,Power |
| 儲(chǔ)藏條件 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 |
勒西韋林(Lersivirine,473921-12-9,UK-453061)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)過(guò)程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類(lèi)存儲(chǔ)，并交于專(zhuān)業(yè)生物廢氣物處理公司處理，以免造成環(huán)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試劑,UK-453061雜質(zhì),UK-453061中間體,UK-453061合成,UK-453061密度,UK-453061閃點(diǎn),UK-453061溶解度,UK-453061旋光度,UK-453061購(gòu)買(mǎi),UK-453061MSDS,
| 產(chǎn)品說(shuō)明 | 勒西韋林(Lersivirine,473921-12-9,UK-453061)是逆轉(zhuǎn)錄酶抑制劑,UK-453061是抗HIV劑. |
| Introduction | 勒西韋林(Lersivirine,473921-12-9,UK-453061)is a reverse transcriptase inhibitor, UK-453061 is an anti-HIV agent. |
| Application1 | Lersivirine（UK-453061）是新一代非核苷類(lèi)逆轉(zhuǎn)錄酶抑制劑（NNRTI，IC50 = 119 nM），具有獨(dú)特的耐藥性，對(duì)野生型人免疫缺陷病毒和臨床相關(guān)的NNRTI耐藥株表現(xiàn)出有效的抗逆轉(zhuǎn)錄病毒活性。 |
| Application2 | Lersivirine（UK-453061）是非核苷逆轉(zhuǎn)錄酶抑制劑（NNRTI），IC50為119 nM，對(duì)野生型和NNRTI抗性型毒株都有效。 |
| Application3 |
勒西韋林(Lersivirine,473921-12-9,UK-453061)藥理學(xué)：
※Lersivirine是下一代吡唑非核苷逆轉(zhuǎn)錄酶抑制劑。Lersivirine保留抗HIV病毒在位置Y181突變，這在賦予抗性活性依非韋倫，依曲韋林和奈韋拉平。
※Lersivirine是正在開(kāi)發(fā)中的用于治療HIV-1感染的下一代非核苷類(lèi)逆轉(zhuǎn)錄酶抑制劑（NNRTI）。它可以防止HIV進(jìn)入健康的CD4細(xì)胞核，從而阻止細(xì)胞產(chǎn)生新病毒并減少體內(nèi)病毒的數(shù)量。
※Lersivirine（UK-453061）是新一代非核苷類(lèi)逆轉(zhuǎn)錄酶抑制劑（NNRTI，IC50 = 119 nM），具有獨(dú)特的耐藥性，對(duì)野生型人免疫缺陷病毒和臨床相關(guān)的NNRTI耐藥株表現(xiàn)出有效的抗逆轉(zhuǎn)錄病毒活性。 ； IC50值：0.119 uM [1]；目標(biāo)：
※NNRTIUK-453061（化合物5）顯示出對(duì)大批野生型和耐藥HIV的優(yōu)異活性，與針對(duì)分離的RT酶的令人鼓舞的特性一致。借助于有效和簡(jiǎn)潔的合成途徑，可以容??易地以克數(shù)制備化合物5。該化合物還具有良好的水溶性和配制特性，
※Lersivirine（UK-453061）是非核苷逆轉(zhuǎn)錄酶抑制劑（NNRTI），IC50為119 nM，對(duì)野生型和NNRTI抗性型毒株都有效。
※Lersivirine（UK-453061）是新一代非核苷類(lèi)逆轉(zhuǎn)錄酶抑制劑（NNRTI，IC50 = 119 nM），具有獨(dú)特的耐藥性，對(duì)野生型人免疫缺陷病毒和臨床相關(guān)的NNRTI耐藥株表現(xiàn)出有效的抗逆轉(zhuǎn)錄病毒活性。IC50值：0.119 uM ,目標(biāo)：NNRTI UK-453061（化合物5）顯示出對(duì)大批野生型和耐藥HIV的優(yōu)異活性，與針對(duì)分離的RT酶的令人鼓舞的特性一致。借助于有效和簡(jiǎn)潔的合成途徑，可以容易地以克數(shù)制備化合物5。該化合物還具有良好的水溶性和配制特性，可進(jìn)一步進(jìn)行體內(nèi)評(píng)估。評(píng)估5（UK-453,061，lersivirine）治療HIV感染潛力的臨床試驗(yàn)正在進(jìn)行中，并將在適當(dāng)?shù)臅r(shí)候報(bào)告進(jìn)一步的進(jìn)展。在臨床相關(guān)的lersivirine劑量（每日總劑量500-1,000 mg）下，咪達(dá)唑侖的平均血漿暴露以劑量依賴(lài)性方式降低20-36％。萊西韋林1,000 mg QD與OC的共同給藥對(duì)PK的影響較小，乙炔雌二醇暴露量增加10％，左炔諾孕酮暴露量減少13％[2]。交配的Crl：CD1（ICR）小鼠在妊娠第6至17天每天口服一次給予0、150、350和500 mg / kg lersivirine，然后在妊娠第18天進(jìn)行剖宮產(chǎn)。大劑量組以250 mg / kg的劑量進(jìn)行，以誘導(dǎo)肝代謝酶.
| 警示圖 | |
| 危險(xiǎn)性 | warning |
| 危險(xiǎn)性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對(duì)身體有害 |
| 安全防護(hù) | P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護(hù)理 |
| 備注 | 實(shí)驗(yàn)過(guò)程中防止吸入、食入，做好安全防護(hù) |
勒西韋林(Lersivirine,473921-12-9,UK-453061)危害標(biāo)識(shí)：
| 象形圖 |  |
| 信號(hào) | Warning |
| GHS危險(xiǎn)說(shuō)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. | |
| 防范說(shuō)明代碼 | P201, P202, P260, P273, P281, P308+P313, P314, P405, and P501 |
| (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 |
勒西韋林(Lersivirine,473921-12-9,UK-453061)參考文獻(xiàn):
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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