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10mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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5g |
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Purity: ≥98%
Fidaxomicin (formerlyOPT-80, PAR-101; PAR101; OPT80; Dificid; Dificlir; Clostomicin B1; Difimicin; Lipiarmycin; Tiacumicin B) is a narrow spectrum macrocyclic antibiotic agent and a naturally occuring fermentation product extracted from the actinomycete Dactylosporangium aurantiacum subspecies hamdenesisthat. As an RNA polymerase inhibitor, fidaxomicin binds to the DNA template–RNA polymerase (RNAP) complex before the open RNAP–DNA complex forms, which is when transcription starts.
Targets |
RNA polymerase
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ln Vitro |
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ln Vivo |
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Animal Protocol |
Male Golden Syrian hamsters (80-100 g, Hamster model for pseudomembranous colitis)
0.2, 1, and 5 mg/kg Orally, once a day for 5 days, beginning 8 h after infection |
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References |
Molecular Formula |
C52H74CL2O18
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Molecular Weight |
1058.04
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Exact Mass |
304.13
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Elemental Analysis |
C, 54.28; H, 5.04; F, 4.52; N, 13.33; O, 22.83
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CAS # |
873857-62-6
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CC[C@H]1/C=C(/[C@H](C/C=C/C=C(/C(=O)O[C@@H](C/C=C(/C=C(/[C@@H]1O[C@H]2[C@H]([C@H]([C@@H](C(O2)(C)C)OC(=O)C(C)C)O)O)\C)\C)[C@@H](C)O)\CO[C@H]3[C@H]([C@H]([C@@H]([C@H](O3)C)OC(=O)C4=C(C(=C(C(=C4O)Cl)O)Cl)CC)O)OC)O)\C
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InChi Key |
ZVGNESXIJDCBKN-UUEYKCAUSA-N
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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
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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-6,6-dimethyl-5-(2-methylpropanoyloxy)oxan-2-yl]oxy-11-ethyl-8-hydroxy-18-[(1R)-1-hydroxyethyl]-9,13,15-trimethyl-2-oxo-1-oxacyclooctadeca-3,5,9,13,15-pentaen-3-yl]methoxy]-4-hydroxy-5-methoxy-2-methyloxan-3-yl] 3,5-dichloro-2-ethyl-4,6-dihydroxybenzoate
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.9451 mL | 4.7257 mL | 9.4514 mL | |
5 mM | 0.1890 mL | 0.9451 mL | 1.8903 mL | |
10 mM | 0.0945 mL | 0.4726 mL | 0.9451 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05201079 | Recruiting | Biological: MBK-01 Drug: Dificlir |
Recurrent Clostridium Difficile Infection Primary Clostridium Difficile Infection |
Mikrobiomik Healthcare Company S.L. |
October 29, 2021 | Phase 3 |
NCT05266807 | Recruiting | Drug: oral capsulized Fecal Microbiota Transplantation Drug: Vancomycin or Fidaxomicin |
Clostridioides Difficile Infection |
Benoit Guery | August 16, 2022 | Phase 3 |
NCT02667418 | Recruiting | Drug: Fidaxomicin Drug: Vancomycin |
Fidaxomicin Difficile |
VA Office of Research and Development |
December 21, 2015 | Phase 4 |
NCT02083627 | Completed | Drug: fidaxomicin BDrug: rosuvastatin |
Intestinal Absorption Healthy Subjects |
Astellas Pharma Europe B.V. | February 2013 | Phase 1 |
NCT01818141 | Active Recruiting |
Drug: Vancomycin Drug: Fidaxomicin |
Clostridium Difficile Infection | Hartford Hospital | October 17, 2012 | Phase 4 |
A, Inhibition of bacterial RNA polymerase (RNAP) by lipiarmycins (including fidaxomicin) occurs following binding of the holoenzyme to the DNA template, but prior to development of the open DNA-RNAP complex [13]. Clin Infect Dis . 2012 Feb 15;54(4):568-74. td> |