西那卡塞作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetCinacalcetCat. No.: HY-70037CAS No.: 226256-56-0分式: CHFN分量: 357.41作靶點(diǎn): CaSR作通路: GPCR/G Protein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 : 100 mg/mL (279.79 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制

2、備儲(chǔ)備液1 mM 2.7979 mL 13.9895 mL 27.9791 mL5 mM 0.5596 mL 2.7979 mL 5.5958 mL10 mM 0.2798 mL 1.3990 mL 2.7979 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。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)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添

3、加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.69 mM); Clear solution此案可獲得 2.75 mg/mL (7.69 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲(chǔ)備

4、液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (7.69 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.75 mg/mL (7.69 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液

5、中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.69 mM); Clear solution此案可獲得 2.75 mg/mL (7.69 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 27.5 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Cinacalcet (AMG 073)種可服的 Ca receptor (CaR) 激動(dòng)劑，于治療管疾病。體內(nèi)研究 Cinacalcet

6、HCl (5 and 10 mg/kg) results in a significant reduction in parathyroid gland weight in 5/6 nephrectomyanimals. In sham animals, Cinacalcet HCl has no effect on parathyroid gland cell proliferation or parathyroid weightcompared with vehicle treatment. There are no differences in serum phosphorus leve

7、ls in Cinacalcet HCl (10, 5, or 1mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6 nephrectomized animals. CinacalcetHCl treatment significantly reduces blood ionized calcium levels in sham animals1. Cinacalcet (30 mg/kg/24 h) leadsto a marked reduction in circulating parat

8、hyroid hormone and a modest reduction in serum Ca. Cinacalcet does notalter UCa when the GHS rats are fed the normal Ca diet but lowers UCa when they are fed the low Ca diet. Cinacalcetdoes not alter U supersaturation with respect to either CaOx or CaHPO4 on either diet2.PROTOCOLAnimal To identify a

9、poptosis in parathyroid glands from 5/6 nephrectomized or sham rats treated with vehicle phosphate-Administration 1 buffered saline (PBS) or cinacalcet HCl (10 mg/kg), nuclear DNA fragmentation is measured in situ using theApoptag System. Briefly, parathyroid gland sections from animals treated with

10、 vehicle or cinacalcet HCl are digestedwith 20 g/mL proteinase K in 0.1 mol/L PBS at room temperature for 15 minutes and incubated with 3% hydrogenperoxide/methanol for 5 minutes to block endogenous peroxidase. Sections are incubated for 1 hour at 37C withterminal deoxynucleotidyl transferase (TdT)

11、to label exposed 3-OH DNA ends with digoxigenin-tagged nucleotides.Digoxigenin-labeled DNA is detected by the immunoperoxidase method. Sections are developed with 3,3-diaminobenzidine (DAB), and the nuclei of apoptotic cells are stained brown. The specificity for apoptosis is verifiedby negative sta

12、ining when distilled water is substituted for TdT.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) J Med Chem. 2015 Apr 9;58(7):2958-66. Oxid Med Cell Longev. 2017;2017:3869561. J Biol Chem. 2016 Oct 28;291(44):23126-23135. Gen Comp Endocrino

13、l. 2018 Oct 1;267:1-8. J Food Sci. 2018 Sep;83(9):2394-2401.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Colloton M, et al. Cinacalcet HCl attenuates parathyroid hyperplasia in a rat model of secondary hyperparathyroidism. Kidney Int. 2005 Feb;67(2):467-76.2. D.A. Bushinsky, et al. Effect of cinacalcet on urine calcium excretion and supersaturation in genetic hypercalciuric stone-forming rats. Kidney Int. 2006May;69(9):1586-92.McePdfHeightCauti