西那卡塞作用机制 - Medchemexpress - MCE中国

1、Product Data SheetCinacalcetCat. No.: HY-70037CAS No.: 226256-56-0分式: CHFN分量: 357.41作靶点: CaSR作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (279.79 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制

2、备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添

3、加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.69 mM); Clear solution此案可获得 2.75 mg/mL (7.69 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备

4、液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (7.69 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.75 mg/mL (7.69 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液

5、中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.69 mM); Clear solution此案可获得 2.75 mg/mL (7.69 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Cinacalcet (AMG 073)种可服的 Ca receptor (CaR) 激动剂，于治疗管疾病。体内研究 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.户使本产品发表的科研献 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