| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
At the highest studied concentration (10 μM), cipragamin (NITD609) is non-toxic to human foreskin fibroblasts (HFF) and inhibits Toxoplasma gondii, with a tachyzoite MIC90 of 5 μM and a MIC50 of 1 μM [1]. At 50 and 500 nM, the most effective inhibitor of early gametocyte growth is ciprgamin (NITD609). The formation of late gametocytes is inhibited by sipragamine in a dose-dependent manner [2]. With ICIC50 values ranging from 0.5 to 1.4 nM, cipragmin (NITD609) demonstrates strong efficacy against a panel of Plasmodium falciparum strains that have been culture-adapted. Like artesunate, sipargamine is active against all isolates of P. falciparum and P. vivax in the low nanomolar range (ICIC50 values consistently <10 nM) [3].
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|---|---|
| ln Vivo |
In malaria mouse models, dipergamin (NITD609) has good pharmacokinetic features and single-dose curative effectiveness. In all treated mice, cipramer (100 mg/kg) totally eradicated Plasmodium berghei infection; a single oral dose of 30 mg/kg produced a 50% partial cure [3].
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| References |
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| Additional Infomation |
Cipargamin has been used in trials studying the treatment of Malaria, Cure Rate, and Plasmodium Falciparum Malaria.
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| Molecular Formula |
C19H14CL2FN3O
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|---|---|
| Molecular Weight |
390.2394
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| Exact Mass |
389.049
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| CAS # |
1193314-23-6
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| PubChem CID |
44469321
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| Appearance |
Light brown to brown solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
621.3±55.0 °C at 760 mmHg
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| Flash Point |
329.6±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.738
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| LogP |
4.61
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
26
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| Complexity |
609
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@H]1CC2=C([C@]3(N1)C4=C(C=CC(=C4)Cl)NC3=O)NC5=CC(=C(C=C25)F)Cl
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| InChi Key |
CKLPLPZSUQEDRT-WPCRTTGESA-N
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| InChi Code |
InChI=1S/C19H14Cl2FN3O/c1-8-4-11-10-6-14(22)13(21)7-16(10)23-17(11)19(25-8)12-5-9(20)2-3-15(12)24-18(19)26/h2-3,5-8,23,25H,4H2,1H3,(H,24,26)/t8-,19+/m0/s1
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| Chemical Name |
(3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methylspiro[1H-indole-3,1'-2,3,4,9-tetrahydropyrido[3,4-b]indole]-2-one
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| Synonyms |
GNF609 KAE609, KAE 609,GNF 609 NITD609, NITD 609, NITD-609, KAE-609, GNF-609
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~128.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (7.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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