| CAS NO: | 873857-62-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 5g | 电议 |
| Molecular Weight (MW) | 1058.04 |
|---|---|
| Formula | C52H74Cl2O18 |
| CAS No. | 873857-62-6 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (94.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name: (2R,3S,4S,5S,6R)-6-({(3E,5E,8S,9E,11S,12R,13E,15E,18S)-12-{[(2R,3S,4R,5S)-3,4-Dihydroxy-5-(isobutyryloxy)-6,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-11-ethyl-8-hydroxy-18-[(1R)-1-hydroxyethyl]-9,13,15- trimethyl-2-oxooxacyclooctadeca-3,5,9,13,15-pentaen-3-yl}methoxy)-4-hydroxy-5-methoxy-2-methyltetrahydro-2H-pyran-3-yl 3,5-dichloro-2-ethyl-4,6-dihydroxybenzoate InChi Key: ZVGNESXIJDCBKN-UUEYKCAUSA-N InChi Code: InChI=1S/C52H74Cl2O18/c1-13-30-22-26(6)33(56)18-16-15-17-31(23-66-51-45(65-12)42(61)44(29(9)67-51)69-49(64)35-32(14-2)36(53)39(58)37(54)38(35)57)48(63)68-34(28(8)55)20-19-25(5)21-27(7)43(30)70-50-41(60)40(59)46(52(10,11)72-50)71-47(62)24(3)4/h15-17,19,21-22,24,28-30,33-34,40-46,50-51,55-61H,13-14,18,20,23H2,1-12H3/b16-15+,25-19+,26-22+,27-21+,31-17+/t28-,29-,30+,33+,34+,40-,41+,42+,43+,44-,45+,46+,50-,51-/m1/s1 SMILES Code: O=C(O[C@@H]1[C@@H](C)O[C@@H](OC/C2=C\C=C\C[C@H](O)/C(C)=C/[C@H](CC)[C@@H](O[C@H]3[C@@H](O)[C@@H](O)[C@H](OC(C(C)C)=O)C(C)(C)O3)/C(C)=C/C(C)=C/C[C@@H]([C@H](O)C)OC2=O)[C@@H](OC)[C@H]1O)C4=C(O)C(Cl)=C(O)C(Cl)=C4CC |
| Synonyms | PAR101; OPT80; PAR 101; OPT-80; PAR-101; OPT 80; Dificid; Dificlir; Clostomicin B1; Difimicin; Lipiarmycin; Tiacumicin B. |
| In Vitro | In vitro activity: Fidaxomicin acts as a RNA polymerase inhibitor by binding to the DNA template–RNA polymerase (RNAP) complex prior to the formation of the open RNAP-DNA complex in which transcription is initiated. Therefore it will inhibit protein synthesis. As a result, apoptosis is triggered in susceptible organisms such as C. difficile. |
|---|---|
| In Vivo | The minimum inhibitory concentration for 90% of organisms for fidaxomicin against C. difficile is 0.9978 to 2 μg/mL. Fidaxomicin is not systemically absorbed as shown by a plasma concentrations below the lower limit of quantification after single-dose or multiple-dose. In contrast, fecal concentrations of fidaxomicin are much higher and are concentration-dependent. Cmax = 2 hours; Tmax = 5.2 ng/mL; AUC = 14 ngohr/mL. Fidaxomicin is hydrolyzed by gastric acid or intestinal microsomes into a less active metabolite (OP-1118). The cytochrome enzyme system are not involved in the metabolism of fidaxomicin. |
| Animal model | N/A |
| Formulation & Dosage | 0.9978 to 2 μg/mL |
| References | Clin Infect Dis. 2012 Feb 15;54(4):568-74. |
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