Cipargamin (Synonyms: NITD609; KAE609)

Name: Cipargamin
Brand: MedChemExpress
SKU: HY-14430
Rating: 5.0 (4 reviews)

Cat. No.: HY-14430 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Cipargamin (NITD609) is an potent antimalarial compound, with an IC₅₀ of appr 1 nM against P. falciparum.

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

Cipargamin Chemical Structure

CAS No. : 1193314-23-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 192	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 192	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 174	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 897	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1435	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Cipargamin

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cipargamin (NITD609) is an potent antimalarial compound, with an IC₅₀ of appr 1 nM against P. falciparum.

IC₅₀ & Target

IC50: 1 nM (P. falciparum)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
BHK-21	CC₅₀	> 25 μM Compound: NITD609	Cytotoxicity against human BHK21 cells after 4 days by XTT assay Cytotoxicity against human BHK21 cells after 4 days by XTT assay	[PMID: 20813948]
C6	CC₅₀	> 50 μM Compound: NITD609	Cytotoxicity against human C6 cells after 4 days by XTT assay Cytotoxicity against human C6 cells after 4 days by XTT assay	[PMID: 20813948]
HepG2	CC₅₀	> 10 μM Compound: KAE609; NITD609	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 4 days by XTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 4 days by XTT assay	[PMID: 31385706]
HepG2	CC₅₀	> 25 μM Compound: NITD609	Cytotoxicity against human HepG2 cells after 4 days by XTT assay Cytotoxicity against human HepG2 cells after 4 days by XTT assay	[PMID: 20813948]
THP-1	CC₅₀	> 10 μM Compound: KAE609; NITD609	Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 4 days by XTT assay Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 4 days by XTT assay	[PMID: 31385706]
THP-1	CC₅₀	14 μM Compound: NITD609	Cytotoxicity against human THP1 cells after 4 days by XTT assay Cytotoxicity against human THP1 cells after 4 days by XTT assay	[PMID: 20813948]

In Vitro

Cipargamin (NITD609) inhibits T. gondii with a MIC₉₀ for tachyzoites of 5 μM and a MIC₅₀ of 1 μM, without toxicity to human foreskin fibroblasts (HFFs) at the highest concentration tested (10 μM)^[1]. Cipargamin (NITD609) is the most effective inhibitor of early gametocyte development at 50 and 500 nM. Cipargamin shows a dose-dependent inhibiting effect on late gametocyte development^[2]. Cipargamin (NITD609) shows potent activities against a panel of culture-adapted P. falciparum strains, with ICIC₅₀ values of 0.5-1.4 nM. Cipargamin is effective as artesunate with potency in the low nanomolar range (ICIC₅₀ values consistently <10 nM) against all P. falciparum and P. vivax isolates^[3].

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

In Vivo

Cipargamin (NITD609) shows favorable pharmacokinetic properties and displays single dose cure efficacy in a malaria mouse model. Cipargamin (100 mg/kg) completely clears P. berghei infection in all treated mice, and partial cure (50%) is achieved with a single oral dose at 30 mg/kg^[3].

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

Clinical Trial

Molecular Weight

390.24

Formula

C₁₉H₁₄Cl₂FN₃O

CAS No.

1193314-23-6

Appearance

Solid

Color

Light brown to brown

SMILES

FC1=C(Cl)C=C(NC2=C3C[C@H](C)N[C@@]2(C4=C(C=CC(Cl)=C4)N5)C5=O)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (128.13 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	2.5625 mL	12.8126 mL	25.6253 mL
5 mM	0.5125 mL	2.5625 mL	5.1251 mL
10 mM	0.2563 mL	1.2813 mL	2.5625 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (7.69 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: ≥98.0%

Select Batch:

Data Sheet (278 KB) SDS (392 KB)

COA (253 KB) HNMR (262 KB) MS (184 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[3]. Rottmann M, et al. Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5625 mL	12.8126 mL	25.6253 mL	64.0631 mL
	5 mM	0.5125 mL	2.5625 mL	5.1251 mL	12.8126 mL
	10 mM	0.2563 mL	1.2813 mL	2.5625 mL	6.4063 mL
	15 mM	0.1708 mL	0.8542 mL	1.7084 mL	4.2709 mL
	20 mM	0.1281 mL	0.6406 mL	1.2813 mL	3.2032 mL
	25 mM	0.1025 mL	0.5125 mL	1.0250 mL	2.5625 mL
	30 mM	0.0854 mL	0.4271 mL	0.8542 mL	2.1354 mL
	40 mM	0.0641 mL	0.3203 mL	0.6406 mL	1.6016 mL
	50 mM	0.0513 mL	0.2563 mL	0.5125 mL	1.2813 mL
	60 mM	0.0427 mL	0.2135 mL	0.4271 mL	1.0677 mL
	80 mM	0.0320 mL	0.1602 mL	0.3203 mL	0.8008 mL
	100 mM	0.0256 mL	0.1281 mL	0.2563 mL	0.6406 mL

Cipargamin Related Classifications

Infection

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:

Cipargamin1193314-23-6NITD609 KAE609NITD 609NITD-609KAE609KAE 609KAE-609ParasiteInhibitorinhibitorinhibit

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Cipargamin (Synonyms: NITD609; KAE609)

Customer Review

Cipargamin Related Antibodies

4 Publications Citing Use of MCE Cipargamin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Cipargamin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Cipargamin Related Classifications

Keywords:

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Customer Review

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