Cipargamin enantiomer
Cipargamin enantiomer (NITD609 enantiomer) is a Plasmodium falciparum inhibitor that can be characterized as a spirotetrahydro β-carboline (1S,3R stereoisomer). Cipargamin enantiomer exerts antiplasmodial activity against Plasmodium falciparum strains NF54 (IC50 of 77 nM) and K1. Cipargamin enantiomer displays low liver microsomal intrinsic clearance in mouse and human systems. Cipargamin enantiomer does not inhibit CYP2C9. Cipargamin enantiomer can be used for the research of malaria.
For research use only. We do not sell to patients.
- CAS No.: 1193314-24-7
- Formula: C19H14Cl2FN3O
- Molecular Weight:390.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
Description
In Vitro
Cipargamin enantiomer (Compound 19b) inhibits the growth of Plasmodium falciparum NF54 strain with an IC50 of 77 nM[1].
Cipargamin enantiomer has low metabolic clearance in human and mouse liver microsomes[1].
Cipargamin enantiomer (≤10.00 μM) does not inhibit CYP2C9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CL |
|---|---|---|---|
| Mice[1] | 5 mg/kg | i.v. | 2.58 mL/min/kg |
Chemical Information
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CAS No. 1193314-24-7
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Molecular Weight 390.24
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Formula C19H14Cl2FN3O
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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 enantiomer; KAE609 enantiomer
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)