2. Metabolic Enzyme/Protease Anti-infection
  3. Dihydroorotate Dehydrogenase Parasite
  4. DSM502

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs.

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

DSM502 Chemical Structure

DSM502 Chemical Structure

CAS No. : 2426616-55-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 440 In-stock
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 640 In-stock
50 mg USD 2150 In-stock
100 mg USD 3250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

DSM502 Related Antibodies

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs[1].

IC50 & Target

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
> 33 μM
Compound: 37; DSM502
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks patch clamp electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks patch clamp electrophysiology assay
[PMID: 32248693]
In Vitro

DSM502 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=20 nM), P. vivax DHODH (PvDHODH, IC50=14 nM) and Pf3D7 cells (EC50=14 nM), with no inhibition of the human enzyme[1].

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

DSM502 Related Antibodies
In Vivo

DSM502 (10 and 50 mg/kg; p.o. once daily for 4 days) results in 97% parasite clearance in confirmatory SCID study compared to 85% clearance in the GSK study[1].
DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t1/2 (2.6, 3.6 h) and Cmax (8.4, 42.3 μM) in mice[1].
DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and Vss (1.2 L/kg) in mice[1].

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

Animal Model: SCID mice (23-36 g) were inoculated with parasites[1]
Dosage: 10 and 50 mg/kg
Administration: P.o. once daily for 4 days starting on day 3 after mice had been inoculated with parasites
Result: Resulted in 97% parasite clearance compared to 85% clearance in the GSK study.
The 10 mg/kg mouse died on day 5.
Molecular Weight

323.31

Formula

C16H16F3N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)C(CC2=CC=C(C(F)(F)F)N=C2)=CN1)NC3CC3
Shipping

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

DMSO : 250 mg/mL (773.25 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 3.0930 mL 15.4650 mL 30.9301 mL
5 mM 0.6186 mL 3.0930 mL 6.1860 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.74%

SDS (251 KB)

COA (246 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
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 3.0930 mL 15.4650 mL 30.9301 mL 77.3252 mL
5 mM 0.6186 mL 3.0930 mL 6.1860 mL 15.4650 mL
10 mM 0.3093 mL 1.5465 mL 3.0930 mL 7.7325 mL
15 mM 0.2062 mL 1.0310 mL 2.0620 mL 5.1550 mL
20 mM 0.1547 mL 0.7733 mL 1.5465 mL 3.8663 mL
25 mM 0.1237 mL 0.6186 mL 1.2372 mL 3.0930 mL
30 mM 0.1031 mL 0.5155 mL 1.0310 mL 2.5775 mL
40 mM 0.0773 mL 0.3866 mL 0.7733 mL 1.9331 mL
50 mM 0.0619 mL 0.3093 mL 0.6186 mL 1.5465 mL
60 mM 0.0516 mL 0.2578 mL 0.5155 mL 1.2888 mL
80 mM 0.0387 mL 0.1933 mL 0.3866 mL 0.9666 mL
100 mM 0.0309 mL 0.1547 mL 0.3093 mL 0.7733 mL
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DSM502 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:

DSM5022426616-55-7DSM 502DSM-502Dihydroorotate DehydrogenaseParasiteDHODHPlasmodiumparasitesInhibitorinhibitorinhibit

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