帕立骨化醇作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetParicalcitolCat. No.: HY-50919CAS No.: 131918-61-1分式: CHO分量: 416.64作靶點(diǎn): VD/VDR作通路: Vitamin D Related儲存式: 4C, protect from light, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (protect from light, stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (240.02 mM; Need u

2、ltrasonic)Ethanol : 12.5 mg/mL (30.00 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.4002 mL 12.0008 mL 24.0015 mL5 mM 0.4800 mL 2.4002 mL 4.8003 mL10 mM 0.2400 mL 1.2001 mL 2.4002 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-

3、80C, 6 months; -20C, 1 month (protect from light, stored under nitrogen)。-80C 儲存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C 儲存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑

4、： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.00 mM); Clear solution此案可獲得 2.5 mg/mL (6.00 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITYPage 1 of 2 www.MedChemE物活性 Paricalcitolvitamin D receptor 的激活劑，于治療繼發(fā)性甲狀旁腺功能亢進(jìn)(分泌過多的甲狀旁腺激素)，該疾病

5、與慢性腎功能衰竭有關(guān)。體外研究 Paricalcitol (310-8 M; HP + PC) produces a significant reduction in calcification relative to the observed in cells inHP medium. Paricalcitol causes a reduction in the levels of nuclear -catenin to a level similar to that observed incontrol cells1.體內(nèi)研究 Paricalcitol (300 ng/kg/day) si

6、gnificantly decreases Tau, and prevents LV dysfunction in mice. Paricalcitol reducesmRNA expression of ANP, fibronectin and collagen III in the TAC-pari mice2.PROTOCOLAnimal After TAC or sham surgery, a subset of the mice is treated with paricalcitol, a selective vitamin D receptor activator,Adminis

7、tration 2 which activates the VDR, at a final dose of 300 ng/kg/day. Paricalcitol is dissolved in a 95% propylene glycol and 5%ethyl alcohol solution. Mice are intraperitoneally injected with paricalcitol (or vehicle only) three times per week onMonday, Wednesday and Friday for five consecutive week

8、s. An established anti-hypertrophic and anti-fibrotictreatment, namely the angiotensin II receptor blocker (ARB) losartan is also included. Previous experiments haveshown it is feasible and efficacious to dissolve losartan in the drinking water at a concentration of 30 mg/kg/day;mice are treated for

9、 five consecutive weeks. So, in total eight groups are studied. Sham (n=10), TAC (n=10), Sham +losartan (Sham-los, n=10), TAC + losartan (TAC-los, n=10), Sham + paricalcitol (Sham-pari, n=10), TAC + paricalcitol(TAC-pari, n=10), Sham + paricalcitol + losartan (Sham-combi, n=10) and TAC + paricalcito

10、l + losartan (TAC-combi,n=10).MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Int J Mol Sci. 2017 Dec 19;18(12). pii: E2764. Biomed Pharmacother. 2020 Feb 21;125:109528. J Pharm Biomed Anal. 2020 Jan 31;182:113139. Am J Med Sci. 2016 Aug;352

11、(2):208-14. Ir J Med Sci. 2018 Feb;187(1):75-84.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Martinez-Moreno JM, et al. In vascular smooth muscle cells paricalcitol prevents phosphate-induced Wnt/beta-catenin activation. Am J Physiol RenalPhysiol. 2012 Aug 8.2. Meems LM, et al. The vitamin D receptor activator paricalcitol prevents fibrosis and diastolic dysfunction in a murine model of pressure overload. JSteroid Biochem Mol Biol. 2012 Jul 16;132(3-5):282-289.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been full