WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206459
CAS#: 1282041-94-4
Description: DSM265 is a long-duration, potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor. DSM265 is potential useful for the prevention and treatment of malaria. DSM265 is the first DHODH inhibitor to reach clinical development for treatment of malaria. DSM265 is highly selective toward DHODH of the malaria parasite Plasmodium, efficacious against both blood and liver stages of P. falciparum, and active against drug-resistant parasite isolates. DSM265 has advantages over current treatment options that are dosed daily or are inactive against the parasite liver stage.
Hodoodo Cat#: H206459
Name: DSM265
CAS#: 1282041-94-4
Chemical Formula: C14H12F7N5S
Exact Mass: 415.07
Molecular Weight: 415.330
Elemental Analysis: C, 40.49; H, 2.91; F, 32.02; N, 16.86; S, 7.72
Synonym: DSM265; DSM-265; DSM 265;
IUPAC/Chemical Name: 2-(1,1-difluoroethyl)-5-methyl-N-(4-(pentafluoro-l6-sulfanyl)phenyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
InChi Key: OIZSVTOIBNSVOS-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H12F7N5S/c1-8-7-11(26-13(22-8)24-12(25-26)14(2,15)16)23-9-3-5-10(6-4-9)27(17,18,19,20)21/h3-7,23H,1-2H3
SMILES Code: FS(F)(F)(F)(C1=CC=C(NC2=CC(C)=NC3=NC(C(F)(F)C)=NN23)C=C1)F
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, not in water
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: | DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. |
| In vitro activity: | TBD |
| In vivo activity: | Liver parasite burden was quantified by IVIS and showed a 2.5-log reduction in liver burden (P < 0.0001) in the DSM265-treated mice compared with control mice (Figure 2, B and C). Whole livers were also harvested on day 6 to determine parasite burden using qPCR. DSM265 resulted in a 5.2-log decrease in liver stage burden (P < 0.0001) (Figure 2D). Additionally, in 3 of the 5 mice treated with DSM265, the number of Plasmodium 18S rRNA copies were below the assay limit of quantification and were completely undetectable in 1 mouse. Reference: JCI Insight. 2018 Jan 11; 3(1): e92587. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5821200/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.0 | 120.39 |
The following data is based on the product molecular weight 415.33 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: | 1. Flannery EL, Foquet L, Chuenchob V, Fishbaugher M, Billman Z, Navarro MJ, Betz W, Olsen TM, Lee J, Camargo N, Nguyen T, Schafer C, Sack BK, Wilson EM, Saunders J, Bial J, Campo B, Charman SA, Murphy SC, Phillips MA, Kappe SH, Mikolajczak SA. Assessing drug efficacy against Plasmodium falciparum liver stages in vivo. JCI Insight. 2018 Jan 11;3(1):e92587. doi: 10.1172/jci.insight.92587. PMID: 29321371; PMCID: PMC5821200. |
| In vitro protocol: | TBD |
| In vivo protocol: | 1. Flannery EL, Foquet L, Chuenchob V, Fishbaugher M, Billman Z, Navarro MJ, Betz W, Olsen TM, Lee J, Camargo N, Nguyen T, Schafer C, Sack BK, Wilson EM, Saunders J, Bial J, Campo B, Charman SA, Murphy SC, Phillips MA, Kappe SH, Mikolajczak SA. Assessing drug efficacy against Plasmodium falciparum liver stages in vivo. JCI Insight. 2018 Jan 11;3(1):e92587. doi: 10.1172/jci.insight.92587. PMID: 29321371; PMCID: PMC5821200. |
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