雷帕霉素
现货促销 25mg/50mg/100mg
Rapamycin
>99% M.W. 914.19 M.F. C51H79NO13 [53123-88-9]RTECS: VE6250000 M.I. 12: 8288
Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO or ethanol (up to about 50 mg/mL for either solvent). Disposal: A
View the MSDS for this product
- 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).
- 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.
- Rapamycin formulations for in vivo use: Many of our customers have asked for information about preparing formulations of rapamycin for administration to animals. Here are several journal citations and links for information on this topic:
- See also our other standard immunosuppressant products:
- Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use
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