WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H562200
CAS#: 1169701-00-1
Description: APX001 is a prodrug of APX-001A, the first-in-class inhibitor of the fungal protein Gwt1.
Hodoodo Cat#: H562200
Name: APX001
CAS#: 1169701-00-1
Chemical Formula: C22H21N4O6P
Exact Mass: 468.12
Molecular Weight: 468.400
Elemental Analysis: C, 56.41; H, 4.52; N, 11.96; O, 20.49; P, 6.61
This product is not in stock, which may be available by custom synthesis.
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Synonym: APX001; APX-001; APX 001;
IUPAC/Chemical Name: (2-amino-3-(3-(4-((pyridin-2-yloxy)methyl)benzyl)isoxazol-5-yl)pyridin-1-ium-1-yl)methyl hydrogen phosphate
InChi Key: JQONJQKKVAHONF-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H21N4O6P/c23-22-19(4-3-11-26(22)15-31-33(27,28)29)20-13-18(25-32-20)12-16-6-8-17(9-7-16)14-30-21-5-1-2-10-24-21/h1-11,13,23H,12,14-15H2,(H2,27,28,29)
SMILES Code: NC1=[N+](COP([O-])(O)=O)C=CC=C1C2=CC(CC(C=C3)=CC=C3COC4=CC=CC=N4)=NO2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 468.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Zhao M, Lepak AJ, VanScoy B, Bader JC, Marchillo K, Vanhecker J, Ambrose PG, Andes DR. In Vivo Pharmacokinetics and Pharmacodynamics of APX001 against Candida spp. in a Neutropenic Disseminated Candidiasis Mouse Model. Antimicrob Agents Chemother. 2018 Jan 29. pii: AAC.02542-17. doi: 10.1128/AAC.02542-17. [Epub ahead of print] PubMed PMID: 29378706.
2: Hager CL, Larkin EL, Long L, Zohra Abidi F, Shaw KJ, Ghannoum MA. In Vitro and In Vivo Evaluation of the Antifungal Activity of APX001A/APX001 against Candida auris. Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: e02319-17. doi: 10.1128/AAC.02319-17. Print 2018 Mar. PubMed PMID: 29311065.
3: Gonzalez-Lara MF, Sifuentes-Osornio J, Ostrosky-Zeichner L. Drugs in Clinical Development for Fungal Infections. Drugs. 2017 Sep;77(14):1505-1518. doi: 10.1007/s40265-017-0805-2. PubMed PMID: 28840541.
4: Osherov N, Kontoyiannis DP. The anti-Aspergillus drug pipeline: Is the glass half full or empty? Med Mycol. 2017 Jan 1;55(1):118-124. Epub 2016 Aug 25. Review. PubMed PMID: 27562862.