2. Anti-infection
  3. Fungal
  4. APX2039

APX2039 is a brain-penetrant and orally active Gwt1 protein inhibitor. APX2039 inhibits an early step in fungal glycosylphosphatidylinositol anchor biosynthesis. APX2039 can be used for the research of cryptococcal meningitis and invasive mycosis caused by Talaromyces marneffei.

For research use only. We do not sell to patients.

APX2039

APX2039 Chemical Structure

CAS No. : 2342606-49-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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APX2039 Related Antibodies

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Description

APX2039 is a brain-penetrant and orally active Gwt1 protein inhibitor. APX2039 inhibits an early step in fungal glycosylphosphatidylinositol anchor biosynthesis. APX2039 can be used for the research of cryptococcal meningitis and invasive mycosis caused by Talaromyces marneffei[1][2][3].

In Vitro

APX2039 (0.008 μg/mL) potently inhibits Cryptococcus neoformans var. grubii H99 in vitro with an MIC of 0.008 μg/mL[1].
APX2039 (0.008-4 µg/mL; 72 h) inhibits growth of clinical Talaromyces marneffei isolates in vitro with a geometric mean MIC of 0.98 µg/mL, an MIC50 of 1 µg/mL, and an MIC90 of 5 µg/mL, with individual MIC values ranging from 0.25 µg/mL to 4 µg/mL[2].
APX2039 (0.002-2 μg/mL; 40-72 h) potently inhibits the growth of Cryptococcus neoformans H99 (MIC = 0.008 μg/mL), Cryptococcus gattii WM276 (MIC = 0.004 μg/mL), Candida albicans 90028 (MIC = 0.031 μg/mL), and Aspergillus fumigatus MYA3626 (MEC = 0.125 μg/mL) in vitro[3].
APX2039 (0.002-2 μg/mL; 72 h) potently inhibits the growth of 18 clinical Cryptococcus neoformans and Cryptococcus gattii isolates (including Fluconazole (HY-B0101)-resistant strains) in vitro, with an MIC range of 0.004 to 0.031 μg/mL and an MIC90 of 0.031 μg/mL[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

APX2039 Related Antibodies
In Vivo

APX2039 (60 mg/kg; p.o.; QD; 7 days) plus ABT (HY-103389) achieves a 6.53 log10 CFU/g reduction in brain fungal burden and 4.45 log10 CFU/g reduction in lung fungal burden in a mouse delayed-treatment model of Cryptococcal meningitis[1].
APX2039 (25-75 mg/kg; p.o.; QD/BID; 13 days) plus ABT at 50 mg/kg p.o. BID achieves a rapid, undetectable CSF fungal burden by day 10 and a 6.6 log10 CFU/g reduction in brain fungal burden in a rabbit model of Cryptococcus meningitis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 (male, 22 to 24 g, infected via tail vein injection with Cryptococcus neoformans strain H99)[1]
Dosage: 60 mg/kg plus 50 mg/kg ABT
Administration: p.o.; QD; 7 days
Result: Reduced mean lung fungal burden by 4.45 log10 CFU/g (from control mean of 5.95 log10 CFU/g to 1.50 log10 CFU/g).
Reduced mean brain fungal burden by 6.53 log10 CFU/g (from control mean of 7.97 log10 CFU/g to 1.44 log10 CFU/g).
Achieved fungal burden below the limit of detection.
Animal Model: New Zealand White (male, 2.3 to 3.1 kg, immunosuppressed with daily hydrocortisone acetate, inoculated via cisterna magna injection with Cryptococcus neoformans strain H99)[1]
Dosage: 25 mg/kg; 50 mg/kg; 75 mg/kg
Administration: p.o.; QD/BID; 13 days
Result: Reduced CSF fungal burden from an average baseline of 4.75 log10 CFU/mL to undetectable levels by day 10 postinfection at 50 mg/kg BID, with a total mean reduction of 4.6 log10 CFU/mL over 8 days of treatment.
Exhibited effective fungicidal activity ranging from -0.53 to -0.66 log10 CFU/mL/day at 50 mg/kg BID.
Reduced brain tissue fungal burden by a mean of 6.6 log10 CFU/g at 50 mg/kg BID, with undetectable levels in cerebellum/brainstem and cerebrum, and demonstrated significantly superior efficacy to fluconazole and amphotericin B (adjusted P = 0.027 for both).
Achieved mean total CSF fungal burden reduction of 2.7 log10 CFU/mL by day 14 at 75 mg/kg QD, with a fungal clearance rate of -0.34 log10 CFU/mL/day.
Achieved mean total CSF fungal burden reduction of 0.72 log10 CFU/mL by day 14 at 50 mg/kg QD, with a fungal clearance rate of -0.06 log10 CFU/mL/day.
Showed no effective reduction at 25 mg/kg QD, with a small mean increase of 0.07 log10 CFU/mL by day 14, equivalent to vehicle control.
Achieved near-maximal antifungal activity with a total drug AUC0-24 of 25 to 50 mg·h/L.
Molecular Weight

362.36

Formula

C20H15FN4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=NC=CC=C1C2=CC(CC3=CC=C(C=C3)OC4=NC(F)=CC=C4)=NO2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (275.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7597 mL 13.7984 mL 27.5969 mL
5 mM 0.5519 mL 2.7597 mL 5.5194 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7597 mL 13.7984 mL 27.5969 mL 68.9922 mL
5 mM 0.5519 mL 2.7597 mL 5.5194 mL 13.7984 mL
10 mM 0.2760 mL 1.3798 mL 2.7597 mL 6.8992 mL
15 mM 0.1840 mL 0.9199 mL 1.8398 mL 4.5995 mL
20 mM 0.1380 mL 0.6899 mL 1.3798 mL 3.4496 mL
25 mM 0.1104 mL 0.5519 mL 1.1039 mL 2.7597 mL
30 mM 0.0920 mL 0.4599 mL 0.9199 mL 2.2997 mL
40 mM 0.0690 mL 0.3450 mL 0.6899 mL 1.7248 mL
50 mM 0.0552 mL 0.2760 mL 0.5519 mL 1.3798 mL
60 mM 0.0460 mL 0.2300 mL 0.4599 mL 1.1499 mL
80 mM 0.0345 mL 0.1725 mL 0.3450 mL 0.8624 mL
100 mM 0.0276 mL 0.1380 mL 0.2760 mL 0.6899 mL
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APX2039 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APX20392342606-49-7APX 2039APX-2039Fungalcryptococcal meningitisAspergillus fumigatus MYA3626invasive mycosisCryptococcus neoformans var. grubii H99Talaromyces marneffeiglycosylphosphatidylinositol anchor biosynthesisblood-brain barrierCryptococcus gattii WM276Gwt1 proteinCandida albicans 90028Inhibitorinhibitorinhibit

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