Cipargamin
Based on 5 publication(s) in Google Scholar
Cipargamin (NITD609) is an potent antimalarial compound, with an IC50 of appr 1 nM against P. falciparum.
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- Purity: 99.90%
- CAS No.: 1193314-23-6
- 화학식: C19H14Cl2FN3O
- 분자량:390.24
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Cipargamin
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Biological Activity
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Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BHK-21 | CC50 |
>25 μM
Compound: NITD609
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Cytotoxicity against human BHK21 cells after 4 days by XTT assay
Cytotoxicity against human BHK21 cells after 4 days by XTT assay
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[PMID: 20813948] |
| C6 | CC50 |
>50 μM
Compound: NITD609
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Cytotoxicity against human C6 cells after 4 days by XTT assay
Cytotoxicity against human C6 cells after 4 days by XTT assay
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[PMID: 20813948] |
| HepG2 | CC50 |
>10 μM
Compound: KAE609; NITD609
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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
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[PMID: 31385706] |
| HepG2 | CC50 |
>25 μM
Compound: NITD609
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Cytotoxicity against human HepG2 cells after 4 days by XTT assay
Cytotoxicity against human HepG2 cells after 4 days by XTT assay
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[PMID: 20813948] |
| THP-1 | CC50 |
>10 μM
Compound: KAE609; NITD609
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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
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[PMID: 31385706] |
| THP-1 | CC50 |
14 μM
Compound: NITD609
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Cytotoxicity against human THP1 cells after 4 days by XTT assay
Cytotoxicity against human THP1 cells after 4 days by XTT assay
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[PMID: 20813948] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1193314-23-6
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Appearance Solid
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분자량 390.24
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화학식 C19H14Cl2FN3O
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Color Yellow to brown
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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
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Synonyms
NITD609; KAE609
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Travel Med Infect Dis
Artemisinin resistance-associated gene mutations in Plasmodium falciparum: A case study of severe malaria from Mozambique. [Abstract]2024 Jan-Feb:57:102684. PMID: 38159875 -
ACS Omega
2019 Jan 31;4(1):2353-2361. PMID: 30729228 -
PLoS Pathog
A single Na+-Pi cotransporter in Toxoplasma plays key roles in phosphate import and control of parasite osmoregulation. [Abstract]2020 Dec 31;16(12):e1009067. PMID: 33383579 -
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용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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.
| 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
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