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      1. 歡迎光臨上海懋康生物科技有限公司
        主頁(yè) > 產(chǎn)品中心 > 生化試劑 > Rapamycin 雷帕霉素 > mz0201Rapamycin雷帕霉素
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        Rapamycin雷帕霉素

        Rapamycin雷帕霉素

        簡(jiǎn)要描述:

        Rapamycin雷帕霉素用途及描述:科研試劑,廣泛應用于分子生物學(xué),藥理學(xué)等科研方面。雷帕霉素(西羅mo司)是目前世界上的強效免疫抑制劑。

        產(chǎn)品時(shí)間:2024-03-21

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        Rapamycin雷帕霉素參數



        Rapamycin (Sirolimus) 雷帕霉素(西羅mo司)

        別  名

        西羅mo司(sirolimus)



        Cas 號

        53123-88-9

        分子式

        C51H79NO13

        分子量

        914.18

        結構式



        Rapamycin雷帕霉素定義:

        一種新型大環(huán)內酯類(lèi)免疫抑制藥物。通過(guò)與相應免疫嗜素RMBP結合抑制細胞周期G0期和G1期,阻斷G1進(jìn)入S期而發(fā)揮作用,其效應為:①抑制T和B細胞增殖;②抑制IL-1、IL-2、IL-6和IFN-γ誘導的淋巴細胞增殖;③抑制IgG和供者特異性抗體(細胞毒抗體)產(chǎn)生;④抑制單核細胞增殖??捎糜诳挂浦才懦夥磻椭委燁?lèi)風(fēng)濕性關(guān)節炎、紅斑狼瘡等自身免疫病。

        溶解性:可溶解于DMSO (50mg/ml)、甲醇(50 mg/ml)、乙醇、丙酮、等有機溶劑;幾乎不溶于水。

        作用

        本品抑制由抗原和細胞因子(白介素IL-2、IL-4和IL-15)激發(fā)的T淋巴細胞的活化和增殖,它亦抑制抗體的產(chǎn)生。在細胞中,西羅mo司與免疫嗜素,即FK結合蛋白-12(FKBP-12)結合,生成FKBP-12免疫抑制復合物。此復合物與哺乳動(dòng)物的西羅mo司BA分子(mTOR,一種關(guān)鍵的調節激酶)結合并抑制其活性,從而抑制細胞周期中G1期向S期的發(fā)展。

        Trusted Worldwide: more than 10,000 vials of our rapamycin have been shipped to more than 2,500 laboratories worldwide since 2002.

        Immunosuppressant, related to FK-506, but without calcineurin inhibitory activity even when complexed to FK-506 binding protein. Selectively blocks signaling that leads to p70 S6 kinase activation (IC50 = 50 pM). Terada, N., et al. "Failure of rapamycin to block proliferation once resting cells have entered the cell cycle despite inactivation of p70 S6 kinase." J. Biol. Chem. 268: 12062-12068 (1993). Fingar, D.C., et al. "Dissociation of pp70 ribosomal protein S6 kinase from insulin-stimulated glucose transport in 3T3-L1 adipocytes." J. Biol. Chem. 268: 3005-3008 (1993). Price, D.J., et al. "Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase." Science 257: 973-977 (1992). Chung, J., et al. "Rapamycin-FKBP specifically blocks growth-dependent activation of and signaling by the 70 kd S6 protein kinases." Cell 69: 1227-1236 (1992).

        Lymphokine-induced cell proliferation at the G1 phase is inhibited and apoptosis in a murine B cell line is induced by rapamycin. Rapamycin arrests the Saccharomyces cerevisiae cell cycle irreversibly in the G1 phase. Morice, W.G. ,et al. "Rapamycin-induced inhibition of p34cdc2 kinase activation is associated with G1/S-phase growth arrest in T lymphocytes." J. Biol. Chem. 268: 3734-3738 (1993). Kay, J.E., et al. "Inhibition of T and B lymphocyte proliferation by rapamycin." Immunology 72: 544-549 (1991). Heitman, J., et al. "Targets for cell cycle arrest by the immunosuppressant rapamycin in yeast." Science 253: 905-909 (1991).

        Rapamycin extended median and maximal lifespan of both male and female mice when fed late in life. Harrison, D.E., et al. "Rapamycin fed late in life extends lifespan in genetically heterogeneous mice." Nature 460: 392-395 (2009).

        Rapamycin has shown activity in slowing cellular and organismal aging. Rapamycin abolished nuclear blebbing, delayed the start of cellular senescence, and improved the degradation of progerin in Hutchinson-Gilford progeria syndrome fibroblast cells. It also reduced the formation of insoluble progerin aggregates and resulted in clearance through autophagic mechanisms in normal fibroblasts. Cao, K., et al. "Rapamycin reverses cellular phenotypes and enhances mutant protein clearance in Hutchinson-Gilford progeria syndrome cells." Sci. Transl. Med. 3: 89ra58 (2011).

        Due to a different mechanism of action than FK506 and other immunosuppressants, rapamycin may prove to be important in organ transplant patient therapy. Fewer side effects than the standard anti-rejection treatments have been observed. Proliferation of activated T cells, but not apoptosis, is blocked by rapamycin. The induction of apoptosis of rejection-causing T cells reduces the tendency towards transplant rejection. Schwarz, C. and Oberbauer, R. "The future role of target of rapamycin inhibitors in renal transplantation." Curr Opin Urol. 12: 109-113 (2002). Wells, A.D. et al. "Requirement for T-cell apoptosis in the induction of peripheral transplantation tolerance." Nat. Med. 5: 1303-1307 (1999). Li, Y., et al. "Blocking both signal 1 and signal 2 of T-cell activation prevents apoptosis of alloreactive T cells and induction of peripheral allograft tolerance." Nat. Med. 5: 1298-1302 (1999).

        We have had one lot of Selleck Chemical's rapamycin analyzed by a highly experienced and expert clinical analytical laboratory that specializes in rapamycin analyses. Using liquid chromatography - mass spectrometry, they found a purity of 96.7% (cis plus trans) for a lot of Selleck's rapamycin. In contrast, we have proven our rapamycin to be greater than 99% in purity for every lot, no exceptions.

        More on the subject of rapamycin purity: HPLC analysis of rapamycin is somewhat complicated. Rapamycin forms several chromatographically separable species in solution, consisting perhaps of different conformers, tautomers, hydrates and/or isomers, but they are all in equilibrium with the major form, trans-rapamycin. We have shown this by collecting the individual impurity peaks in our rapamycin product and individually re-injecting them into the HPLC. In each case, upon re-injection the collected impurity peak is reduced or absent, and the major peak is again trans-rapamycin, of ~95% purity or higher, thus confirming re-equilibration back to the major trans-isomer of rapamycin. Because we find that all significant impurities (generally, those above 0.1%) in our product, including the cis-isomer, are in equilibrium with the trans isomer in the solution used for analysis, the actual purity of our product is >99% rapamycin, in all of its equilibrium forms. In contrast, material from other suppliers typically contains impurities that do not equilibrate with trans-rapamycin, and thus are genuine contaminants. These results also indicate that it is probably not possible to obtain the trans isomer in pure form, because in solution it will quickly re-equilibrate to the mixture of cis and trans.

        儲存條件:-20℃,避光防潮密閉干燥。


        訂購信息:

        品名

        產(chǎn)地

        貨號

        規格

        單價(jià)

        備注

        Rapamycin (Sirolimus) 雷帕霉素(西羅mo司)

        MKbio

        MZ0201-10MG

        10MG

        248

        現貨

        Rapamycin (Sirolimus) 雷帕霉素(西羅mo司)

        MKbio

        MZ0201-100MG

        100MG

        680

        現貨

        上海懋康生物科技有限公司是一家涉足于生命科學(xué)和生物技術(shù)領(lǐng)域研究的試劑、儀器和實(shí)驗室消耗品與實(shí)驗服務(wù)工作,主要從事細胞生物學(xué)、植物學(xué)、分子生物學(xué)、免疫學(xué)、生物化學(xué)、蛋白組學(xué)。生物制藥與診斷試劑研發(fā)生產(chǎn)等領(lǐng)域。 本公司秉承“以人為本,以誠為信、合同守信"的經(jīng)營(yíng)理念。堅持"品質(zhì)保障"的原則為廣大客戶(hù)提供優(yōu)質(zhì)產(chǎn)品。
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