Art. -Nr.: HY-132171A

DSM705 hydrochloride

Name: DSM705 hydrochloride
Brand: MedChemExpress
SKU: HY-132171A
Price: 260.00 USD
Availability: InStock
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DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC₅₀=95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs.

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Reinheit : 98.22%
CAS. Nr.: 2989908-08-7
Formel: C₁₉H₂₀ClF₃N₆O
Molecular Weight:440.85

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DSM705 hydrochloride Chemical Structure

CAS. Nr.: 2989908-08-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Plasmodium

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In Vitro

DSM705 hydrochloride shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC₅₀=95 nM), P. vivax DHODH (PvDHODH, IC₅₀=52 nM) and Pf3D7 cells (EC₅₀=12 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.

In Vivo

DSM705 (3-200 mg/kg; p.o. twice a day for 6 days) hydrochloride provides the maximum rate of parasite killing at the dose of 50 mg/kg and fully suppresses parasitemia by days 7-8^[1].
DSM705 (2.6 and 24 mg/kg; a single p.o.) hydrochloride exhibits high oral bioavailability (74%, 70%), apparent t_1/2 (3.4, 4.5 h) and C_max (2.6, 20 μM) in Swiss outbred mice^[1].
DSM705 (2.3 mg/kg; a single i.v.) hydrochloride exhibits plasma clearance (CL=2.8 mL/min/kg) and V_ss (1.3 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 were inoculated with parasites^[1]
Dosage:

3, 10, 20, 50, 100, 200 mg/kg
Administration:

P.o. twice a day for 6 days
Result:

Killed parasite in a dose dependent manner and fully suppressed parasitemia by days 7-8.

Animal Model:

Swiss Outbred Mice^[1]
Dosage:

2.6 and 24 mg/kg for p.o.; 2.3 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:

A single p.o. and i.v.
Result:

P.o.: F=74/70%, t_1/2=3.4/4.5 h, C_max=2.6/20 μM.
I.v.: CL=2.8 mL/min/kg, V_ss=1.3 L/kg.

Chemical Information

CAS. Nr. 2989908-08-7
Appearance Solid
Molecular Weight 440.85
Formel C₁₉H₂₀ClF₃N₆O
Color White to off-white
SMILES

C[C@H](C1=NC=NN1)NC(C2=C(C(C3(C4=CC=C(N=C4)C(F)(F)F)CC3)=CN2)C)=O.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

Methanol : 250 mg/mL (567.09 mM; Need ultrasonic)

DMSO : 100 mg/mL (226.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2683 mL

11.3417 mL

22.6835 mL

5 mM

0.4537 mL

2.2683 mL

4.5367 mL

10 mM

0.2268 mL

1.1342 mL

2.2683 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Palmer MJ, et, al. Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem. 2021 May 13;64(9):6085-6136. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Methanol	1 mM	2.2683 mL	11.3417 mL	22.6835 mL	56.7086 mL
	5 mM	0.4537 mL	2.2683 mL	4.5367 mL	11.3417 mL
	10 mM	0.2268 mL	1.1342 mL	2.2683 mL	5.6709 mL
	15 mM	0.1512 mL	0.7561 mL	1.5122 mL	3.7806 mL
	20 mM	0.1134 mL	0.5671 mL	1.1342 mL	2.8354 mL
	25 mM	0.0907 mL	0.4537 mL	0.9073 mL	2.2683 mL
	30 mM	0.0756 mL	0.3781 mL	0.7561 mL	1.8903 mL
	40 mM	0.0567 mL	0.2835 mL	0.5671 mL	1.4177 mL
	50 mM	0.0454 mL	0.2268 mL	0.4537 mL	1.1342 mL
	60 mM	0.0378 mL	0.1890 mL	0.3781 mL	0.9451 mL
	80 mM	0.0284 mL	0.1418 mL	0.2835 mL	0.7089 mL
	100 mM	0.0227 mL	0.1134 mL	0.2268 mL	0.5671 mL

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DSM705 hydrochloride

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