Home Microbiology Parasite inhibitor DDD107498 For research use only.

DDD107498

Synonyms: M-5717, DDD-498

DDD107498 (M-5717, DDD-498) is a P. falciparum translation elongation factor 2 inhibitor. DDD107498 exhibits a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite.

DDD107498 Chemical Structure

DDD107498 Chemical Structure

CAS: 1469439-69-7

Purity & Quality Control

Batch: S008101 DMSO] 93 mg/mL] false] Water] 93 mg/mL] false] Ethanol] Insoluble] false Purity: 98.77%
98.77

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Biological Activity

Description DDD107498 (M-5717, DDD-498) is a P. falciparum translation elongation factor 2 inhibitor. DDD107498 exhibits a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite.
In vitro
In vitro

DDD107498 shows excellent activity against 3D7 parasites, with no toxic to human cells (MRC5 and Hep-G2 cells) at much higher concentrations.[1]
Cell Research Cell lines 3D7, HepG2 and MRC5 cells
Concentrations 0.0001-10 μM
Incubation Time --
Method

--
In Vivo
In vivo

There is a lag of about 24-48 h, during which time the effects of DDD107498 are reversible following wash-out. Rapid killing occurred after parasites when exposed to DDD107498 for more than 48 h.[1]
Animal Research Animal Models NOD-scid IL-2R_null mice
Dosages 0.95 mg/kg/day
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04250363 Completed Healthy Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany February 17 2020 Phase 1
NCT03261401 Completed Healthy Merck KGaA Darmstadt Germany September 15 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 462.56 Formula

C27H31FN4O2
CAS No. 1469439-69-7 SDF --
Smiles C1CCN(C1)CCNC(=O)C2=CC(=NC3=C2C=C(C=C3)F)C4=CC=C(C=C4)CN5CCOCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (201.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 93 mg/mL

Ethanol : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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