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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 1282041-94-4 Chemical Structure| 1282041-94-4

Structure of DSM265
CAS No.: 1282041-94-4

Chemical Structure| 1282041-94-4

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DSM265 is an effective Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor with an IC50 of 8.9 nM, also capable of inhibiting Pf3D7 growth (EC50 = 4.3 nM), suitable for malaria treatment research.

4.5 *For Research Use Only !

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Product Details of DSM265

CAS No. :1282041-94-4
Formula : C14H12F7N5S
M.W : 415.33
SMILES Code : FS(C1=CC=C(NC2=CC(C)=NC3=NC(C(F)(F)C)=NN23)C=C1)(F)(F)(F)F
MDL No. :MFCD28502125

Safety of DSM265

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301+H311+H331-H315-H319
Precautionary Statements:P501-P261-P270-P271-P264-P280-P337+P313-P305+P351+P338-P361+P364-P332+P313-P301+P310+P330-P302+P352+P312-P304+P340+P311-P403+P233-P405
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
rabbit cornea SIRC cells 20 μM 48 hours Evaluate the inhibitory effect of DSM265 on rabbit DHODH, results showed no significant change in DHO levels. Biochem Pharmacol. 2022 Oct;204:115237
human T lymphocyte Jurkat cells 20 μM 48 hours Evaluate the inhibitory effect of DSM265 on human DHODH, results showed no significant change in DHO levels. Biochem Pharmacol. 2022 Oct;204:115237
mouse T lymphocyte EL4 cells 5 μM 48 hours Evaluate the inhibitory effect of DSM265 on mouse DHODH, results showed no significant change in DHO levels. Biochem Pharmacol. 2022 Oct;204:115237
Plasmodium falciparum NF54 liver-stage parasites 0.0057 μg/mL Evaluate the inhibitory effect of DSM265 on liver-stage parasites, showing effective inhibition of parasite growth Sci Transl Med. 2015 Jul 15;7(296):296ra111
Plasmodium falciparum 3D7 0.0018 μg/mL 72 hours Evaluate the inhibitory effect of DSM265 on the blood stage of malaria parasites, showing efficacy against all tested strains Sci Transl Med. 2015 Jul 15;7(296):296ra111
Plasmodium falciparum Pf3D70087/N9 30 to 200 nM 2 months Studied resistance development under continuous drug pressure, found stronger resistance phenotypes Sci Transl Med. 2019 Dec 4;11(521):eaav1636
Plasmodium falciparum 3D7 A10 EC99 6 to 8 days Investigated the development of resistance to DSM265 in malaria parasites, found rapid emergence of resistance Sci Transl Med. 2019 Dec 4;11(521):eaav1636
Plasmodium falciparum Dd2 0.023-0.060 μM 72 hours To evaluate the mechanisms of DSM265 resistance in vitro, results showed that various amino acid changes led to reduced efficacy of DSM265 against the parasite. ACS Infect Dis. 2019 Jan 11;5(1):90-101
Plasmodium falciparum (3D7 clone) 5.93 ±0.78 nM 48 hours Comparison of DSM265 susceptibility between Plasmodium falciparum and Plasmodium knowlesi, showing P. falciparum is significantly more susceptible to DSM265 than P. knowlesi. Int J Parasitol Drugs Drug Resist. 2021 Dec;17:5-11
Plasmodium knowlesi (A1-H.1 clone) 44.9 ±9.49 nM 27 hours Comparison of DSM265 susceptibility between Plasmodium knowlesi and Plasmodium falciparum, showing P. knowlesi is significantly less susceptible to DSM265 than P. falciparum. Int J Parasitol Drugs Drug Resist. 2021 Dec;17:5-11

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD-scid IL-2Rγnull mice Plasmodium falciparum-infected SCID mouse model Oral 3 mg/kg/day Twice daily for 4 days Evaluate the antimalarial efficacy of DSM265 in vivo, showing significant antimalarial activity Sci Transl Med. 2015 Jul 15;7(296):296ra111
FRG huHep mice Liver-chimeric humanized mouse model Oral 20 mg/kg Administered at 2, 24, and 48 hours post-infection To assess the efficacy of DSM265 against P. falciparum liver stages, showing a significant reduction in liver parasite burden. JCI Insight. 2018 Jan 11;3(1):e92587
NOD-scid IL2Rγnull mice P. falciparum infection model Oral 50 mg/kg Once daily for 4 days Evaluated resistance development in a mouse model, found similar resistance mutations as in vitro Sci Transl Med. 2019 Dec 4;11(521):eaav1636
SCID mice P. falciparum SCID mouse malaria model Oral 10 and 30 mg/kg Once daily for 4 days To evaluate the in vivo antimalarial activity of the compounds, results showed that compound 9 had the most potent in vivo activity. J Med Chem. 2016 Jun 9;59(11):5416-31
Mice CD-1 mice Oral 300 mg/kg/day Once daily for 10 days Evaluate the pharmacodynamics of DSM265 in mice, results showed no significant change in DHO levels in blood and urine. Biochem Pharmacol. 2022 Oct;204:115237
SCID mice SCID mouse model Oral 10, 20, 30, 40, 50, 60 mg/kg Once daily for 4 days To evaluate the antimalarial efficacy of DSM265 in the SCID mouse model, the results showed that DSM265 significantly reduced parasitemia at a dose of 60 mg/kg. ACS Omega. 2018 Aug 31;3(8):9227-9240

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.04mL

2.41mL

1.20mL

24.08mL

4.82mL

2.41mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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