Lumicitabine-ALS-008176-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELumicitabineCat. No.: HY-12983ACAS No.: 1445385-02-3Synonyms: ALS-008176; ALS-8176分式: CHClFNO分量: 433.86作靶點(diǎn): RSV作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (1

2、15.24 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.3049 mL 11.5245 mL 23.0489 mL5 mM 0.4610 mL 2.3049 mL 4.6098 mL10 mM 0.2305 mL 1.1524 mL 2.3049 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果

3、的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.76 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.76 mM); Clear solution1/2 Master of Small Molecules

4、您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.76 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Lumicitabine (ALS-008176)是呼吸道合胞病毒（RSV）聚合酶的抑制劑。體外研究 Lumicitabine is an orally bioavailable prodrug of the novel RSV replication inhibitor ALS-008112, a cytidinenucleoside analog

5、ue 1.體內(nèi)研究 Lumicitabine demonstrates excellent anti-RSV efficacy and safety in a phase 2 clinical RSV challenge study.It exhibits good oral bioavailability and a high level of 2c-TP in vivo. Lumicitabine has excellent stabilityprofiles in formulations (24 h storage stability in 0.5% methylcellulose a

6、queous formulation at rt) andsimulats gastric and intestinal fluids (half-life 2 h). Its solubility is adequate to support oral administration insolutions with relatively low percentage of organic solvent and in aqueous suspensions. High levels of NMPand NTP are obtained following oral administratio

7、n of Lumicitabine to monkeys 2. In an adult humanchallenge study, Lumicitabine has shown efficacy against RSV infection 1.PROTOCOLAnimal Rats: Lumicitabine are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies areAdministration 2 conducted at 5 mg/kg and for oral PK studies t

8、he prodrugs are administered at 5 mg/kg parent nucleosideequivalent doses. Blood samples are typically collected at various time points up to 24 h post dose for rat 2.Monkeys: Lumicitabine are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies areconducted at 5 mg/kg and for o

9、ral PK studies the prodrugs are administered at 5 mg/kg parent nucleosideequivalent doses. Blood samples are typically collected at various time points up to 12 h post dose forMonkeys 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. DeVinc

10、enzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov19;373(21):2048-58.2. Wang G, et al. Discovery of 4-chloromethyl-2-deoxy-3,5-di-O-isobutyryl-2-fluorocytidine (ALS-8176), a first-in-class RSV polymeraseinhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78.McePdfHeightCaution: Product has not been fully