Azoffluxin
Azoffluxin (CMLD012336) is a Cdr1 inhibitor. Azoffluxin enhances the activity of Fluconazole (HY-B0101) and other intracellular-acting antifungal agents against drug-resistant Candida. Azoffluxin is used for research on fungal efflux-mediated azole resistance and combined antifungal therapy.
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- No. CAS: 2883514-82-5
- Fòrmula: C34H34FNO9
- Peso molecular:619.63
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
Azoffluxin (CMLD012336) (50 μM; 48 h) acts synergistically with Fluconazole (HY-B0101) against the azole-resistant C. auris clade I strain Ci6684, with a FICI of 0.25[1].
Azoffluxin (50 μM; 24 h) reduces the Fluconazole MIC of azole-resistant C. auris by > 8-fold on YPD agar, from > 256 μg/mL to 32 μg/mL[1].
Azoffluxin (50 μM) enhances the activity of Fluconazole against the azole-resistant C. auris clade I strain Ci6684 in a Cdr1-dependent manner[1].
Azoffluxin (25 μM; 24 h) enhances the activity of intracellular-acting compounds (gepinacin, cerulenin, cycloheximide) against the azole-resistant C. auris clade I strain Ci6684 to a level comparable to that of CDR1 knockout, but does not affect the strain's sensitivity to extracellular-acting compounds (caspofungin, amphotericin B)[1].
Azoffluxin (50 μM; 24 h) exerts a synergistic effect with Fluconazole in C. auris clades I, II, and IV, but shows no such effect in clade III isolates B11221 and B11222[1].
Azoffluxin (50 μM; 24 h) exerts a synergistic effect with Fluconazole against C. auris clade III isolate B12037 (FICI = 0.04), and this effect is dependent on Cdr1[1].
Azoffluxin (50 μM; 24 h) acts synergistically with Fluconazole in the azole-resistant clinical isolate Candida albicans CaCi-17 in a Cdr1-dependent manner (FICI = 0.31), but fails to enhance the activity of Fluconazole in the azole-sensitive clinical isolate CaCi-2[1].
Azoffluxin (50 μM; 24 h) slightly enhances the activity of Fluconazole against C. albicans strains carrying gain-of-function TAC1 mutations, but exerts no such effect on azole-sensitive parental strains[1].
Azoffluxin enhances the efficacy of azole drugs against drug-resistant Candida auris strains by inhibiting the Cdr1 efflux pump and increasing the intracellular accumulation of azole drugs[2].
Azoffluxin enhances the efficacy of Fluconazole against azole-resistant Candida albicans isolates[2].
Azoffluxin (1.56 μM; 18 h) enhances the sterol-regulating effect of low-concentration Fluconazole on the azole-resistant C. auris clade I strain Ci6684[1].
Azoffluxin (1.56 μM; 1 h) increases the intracellular accumulation of triazole antifungals by approximately 2.5-fold in the azole-resistant C. auris clade I strain Ci6684[1].
Azoffluxin (1.56-25 μM) upregulates the transcription levels of CDR1 and CDR4-1 in a concentration-dependent manner in the azole-resistant C. auris clade I strain Ci6684, with the strongest inductive effect observed when combined with triazole antifungal agents[1].
Azoffluxin (50 μM; 10 min) increases the accumulation of Nile Red (HY-D0718) in C. auris[1].
Azoffluxin (50 μM; 10 min) increases Nile Red accumulation in the azole-resistant clinical isolate C. albicans CaCi-17, and this effect does not decrease significantly in the cdr1Δ/cdr1Δ strain[1].
Azoffluxin (6.25 μM; 1 h) increases the intracellular accumulation of Nile Red in CaCi-17, a clinical isolate of azole-resistant C. albicans, but exerts no such effect on SN95, an azole-sensitive strain; in contrast, Fluconazole enhances the intracellular accumulation of Azoffluxin in both of the above-mentioned strains[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2β | Tmax | Cmax | AUClast | Vz-F_obs | ClF_obs | MRTlast |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 155.93 min | 60.00 min | 1036.50 ng/mL | 216756.10 min·ng/mL | 10374.51 mL/kg | 46.12 mL/min/kg | 132.73 min |
In Vivo
Azoffluxin (10 mg/kg; i.p.; twice daily for 4 consecutive days) is well tolerated in neutropenic ICR (CD-1) mice, with a 100% survival rate within 21 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (CD-1) (female, 6-week-old, 23 to 27 g, neutropenic, infected intravenously with azole-resistant C. auris clade IV isolate B11801)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 6 hours; 96 hours
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Result:Reduced kidney fungal burden compared to untreated mice.
Enhanced Fluconazole's activity, leading to a greater reduction in kidney fungal burden than either treatment alone.
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Animal Model:ICR (CD-1) (female, ~25 g, neutropenic)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice daily for 4 days
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Result:Showed no physical signs of acute systemic toxicity during 4 days of treatment.
Maintained 100% survival for 21 days post-treatment.
Chemical Information
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No. CAS 2883514-82-5
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Peso molecular 619.63
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Fòrmula C34H34FNO9
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SMILES
O=C1NC2=C(C=CC(F)=C2)C1(C3=C(OC[C@H](O)CC(C)=C)C=C(OCO4)C4=C3)C5=C(OC[C@H](O)CC(C)=C)C=C(OCO6)C6=C5
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Synonyms
CMLD012336
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Azoffluxin Related Classifications
HY-187652 Related Classifications
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