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Cipargamin

Catalog No. T16326 CAS 1193314-23-6

Synonyms: NITD609, KAE609

Cipargamin is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum.

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Cipargamin, CAS 1193314-23-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Cipargamin is an effective antimalarial compound. It has an IC50 of appr 1 nM against P. falciparum.
Targets&IC50	P. falciparum:1 nM
In vitro	Cipargamin is the most effective inhibitor of early gametocyte development at 50 and 500 nM. Cipargamin displays a dose-dependent inhibiting effect on late gametocyte development. Cipargamin inhibits T. gondii with an MIC90 for tachyzoites of 5 μM and an MIC50 of 1 μM. At the highest concentration tested (10 μM), It has no toxicity to human foreskin fibroblasts (HFFs). Cipargamin shows effective activities against a panel of culture-adapted P. falciparum strains (IC50: 0.5-1.4 nM). Cipargamin is effective as an artesunate with potency in the low nanomolar range (ICIC50 values consistently <10 nM) against all P. falciparum and P. vivax isolates [1][2][3].
In vivo	Cipargamin (100 mg/kg) fully clears P. berghei infection in all treated mice, and partial cure (50%) is achieved with a single oral dose at 30 mg/kg. Cipargamin displays favorable pharmacokinetic properties and shows single-dose cure efficacy in a malaria mouse model [3].

Synonyms	NITD609, KAE609
Molecular Weight	390.24
Formula	C19H14Cl2FN3O
CAS No.	1193314-23-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 50 mg/mL (128.13 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zhou Y, et al. Spiroindolone that inhibits PfATPase4 is a potent, cidal inhibitor of Toxoplasma gondii tachyzoites in vitro and in vivo. Antimicrob Agents Chemother. 2014;58(3):1789-92. 2. van Pelt-Koops JC, et al. The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vector. Antimicrob Agents Chemother. 2012 Jul;56(7):3544-8. 3. Rottmann M, et al. Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

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Step Two: Enter the in vivo formulation

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Calculation results:

Working concentration: mg/ml;

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
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The answer of 19.713 mg appears in the Mass box

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Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Molecule Formula

Molecular Weight g/mol

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Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Cipargamin 1193314-23-6 Microbiology/Virology Parasite KAE 609 KAE-609 inhibit NITD609 NITD-609 NITD 609 KAE609 Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.