[CAS NO. 1029939-86-3] Artefenomel

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PRODUCTS SPECIFICATIONS [1029939-86-3]

Catalog

HY-16762

Brand

MCE

CAS

1029939-86-3

DESCRIPTION [1029939-86-3]

Overview

MDL	-
Molecular Weight	469.61
Molecular Formula	C28H39NO5
SMILES	[H][C@@]1(C[C@H](C2)C3)C4([C@@]3([H])C[C@H]2C1)O[C@]5(OO4)CC[C@H](CC5)C6=CC=C(C=C6)OCCN7CCOCC7

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

Summary

Artefenomel (OZ439) is an orally active, synthetic anti-malarial compound containing an artemisinin pharmacophore with a mechanism of action similar to that of artemisinin. Artefenomel has antiviral activity against SARS-CoV-2 ^[1] ^[2] .

In Vitro

Artefenomel (OZ439) (10 μg/mL, 2 h) can alkylate Plasmodium falciparum proteins ^[1] .
Artefenomel (0.3-300 μM) reduces ACE2 expression in Vero cells in a dose-dependent manner and does not induce any cytotoxicity at concentrations up to 300 μM ^[2] .
Artefenomel (33-100 μM) can completely prevent the virus-induced CPE and inhibit SARS-CoV-2 in a dose-dependent manner with an IC ₅₀ of 2.9 µM ^[2] .
Artefenomel (0-10 µg/mL) affects red blood cells and induces anaemia, thereby inducing histological changes (cell death) and macroscopic abnormalities in the embryo from pregnant Crl:CD(SD)BR rats ^[3] .

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

Cell Viability Assay ^[3]

Cell Line:	embryos from pregnant Crl:CD(SD)BR rats
Concentration:	0.1, 1, 2, 5, 7.5, and 10 µg/mL
Incubation Time:
Result:	Showed a slightly shortened tail or slightly delayed telencephalic vesicles at 5 μg/mL, a decrease in the number of circulating red blood cells at 7.5 μg/mL and an arrhythmogenic heartbeat at 10 μg/mL.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02431650	Medicines for Malaria Venture\|Q-Pharm Pty Limited\|Clinical Network Services (CNS) Pty Ltd\|Sullivan Nicolaides Pathology\|QIMR Berghofer Medical Research Institute\|Army Malaria Institute, Australia	Malaria	April 2015	Phase 1\|Phase 2
NCT01958619	Medicines for Malaria Venture\|Richmond Pharmacology Limited	Malaria	October 2013	Phase 1
NCT01383096	Medicines for Malaria Venture\|Nucleus Network Ltd\|Syneos Health	Healthy Volunteers	April 2012	Phase 1
NCT02497612	Sanofi\|Medicines for Malaria Venture	Plasmodium Falciparum Infection	July 25, 2015	Phase 2
NCT04069221	Medicines for Malaria Venture	Malaria	February 28, 2017	Phase 1
NCT02083406	Medicines for Malaria Venture\|Quotient Clinical	Malaria	July 2014	Phase 1
NCT01713608	Medicines for Malaria Venture	Malaria	November 2012	Phase 1
NCT02083380	Medicines for Malaria Venture	Uncomplicated Plasmodium Falciparum Malaria	July 2014	Phase 2\|Phase 3
NCT01660022	Medicines for Malaria Venture\|Cross Research S.A.	Healthy	September 2012	Phase 1
NCT02573857	Medicines for Malaria Venture\|Clinical Network Services (CNS) Pty Ltd\|Q-Pharm Pty Limited\|Queensland Institute of Medical Research	Malaria	October 2015	Phase 1\|Phase 2
NCT02389348	Medicines for Malaria Venture\|Q-Pharm Pty Limited\|QIMR Berghofer Medical Research Institute\|Clinical Network Services (CNS) Pty Ltd	Malaria	February 2015	Phase 1\|Phase 2
NCT01615822	Medicines for Malaria Venture\|University of Cape Town	Malaria	August 2012	Phase 1
NCT02387580	Medicines for Malaria Venture\|Quotient Clinical	Malaria	April 2015	Phase 1
NCT01213966	Medicines for Malaria Venture\|Mahidol University	Malaria, Falciparum\|Malaria, Vivax	October 2010	Phase 2
NCT01732588	Medicines for Malaria Venture	Healthy Volunteers	November 2012	Phase 1
NCT02453581	Medicines for Malaria Venture\|Queensland Institute of Medical Research	Malaria	September 2012	Phase 1
NCT01853475	Medicines for Malaria Venture\|Richmond Pharmacology Limited	Malaria	April 2013	Phase 1
NCT01713621	Medicines for Malaria Venture	Malaria	March 2013	Phase 2
NCT00928083	Medicines for Malaria Venture	Malaria Falciparum\|Malaria Vivax\|Healthy Volunteers	April 2009	Phase 1
NCT03660839	Sanofi\|Medicines for Malaria Venture	Plasmodium Falciparum Infection	September 11, 2018	Phase 2
NCT03542149	Medicines for Malaria Venture\|QIMR Berghofer Medical Research Institute\|Clinical Network Services (CNS) Pty Ltd\|Q-Pharm Pty Limited	Malaria	April 23, 2018	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 4.2 mg/mL ( 8.94 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1294 mL	10.6471 mL	21.2943 mL
5 mM	0.4259 mL	2.1294 mL	4.2589 mL
10 mM	---	---	---

* Please refer to the solubility information to select the appropriate solvent.