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Art. -Nr.: HY-187652

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Azoffluxin

Name: Azoffluxin
Brand: MedChemExpress
SKU: HY-187652
Availability: PreOrder

(Synonyms: CMLD012336)

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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CAS. Nr.: 2883514-82-5
Formel: C₃₄H₃₄FNO₉
Molecular Weight:619.63

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Azoffluxin Chemical Structure

CAS. Nr.: 2883514-82-5

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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	T_1/2β	T_max	C_max	AUC_last	V_{z-F_obs}	Cl_{F_obs}	MRT_last
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 (CMLD012336) (10 mg/kg; i.p.; once every 6 hours; for 96 hours) reduces the systemic C. auris fungal load in neutropenic mice and enhances the antifungal activity of Fluconazole (HY-B0101)^[1].
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.

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]
Dosage:

10 mg/kg
Administration:

i.p.; every 6 hours; 96 hours
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.

Animal Model:

ICR (CD-1) (female, ~25 g, neutropenic)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice daily for 4 days
Result:

Showed no physical signs of acute systemic toxicity during 4 days of treatment.
Maintained 100% survival for 21 days post-treatment.

Chemical Information

CAS. Nr. 2883514-82-5
Molecular Weight 619.63
Formel C₃₄H₃₄FNO₉
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
Synonyms

CMLD012336
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Iyer KR, et al. An oxindole efflux inhibitor potentiates azoles and impairs virulence in the fungal pathogen Candida auris. Nature communications. 2020 Dec 22;11(1):6429.

[2]. Iyer KR, et al. Exploiting Diverse Chemical Collections to Uncover Compounds with Novel Activity Against Human Fungal Pathogens. University of Toronto (Canada) ProQuest Dissertations & Theses, 2021. 28713496.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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