KDU691 |
| Catalog No.GC32118 |
KDU691, une imidazopyrazine dotée d'une puissante activité antiparasitaire contre les schizontes au stade sanguin, les gamétocytes et les stades hépatiques, est un inhibiteur de Plasmodium PI4K.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1513879-19-0
Sample solution is provided at 25 µL, 10mM.
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KDU691 is a PI4K inhibitor.
During the 5 days of dosing, no major weight changes are observed in the animals that receive KDU691 as prophylactic treatment (group 691-proph). From the fourth day of dosing, the animals that are treated with KDU691 show a transient yellow skin color. The KDU691 radical-cure group (group 691-RC) becomes blood-stage positive again at 31.8±0.5 days p.i. (range, 31 to 32 days). Clinical chemistry analysis of the group 691-RC monkeys reveals that bilirubin levels accumulate during the 5-day radical-cure treatment with KDU691[1].
[1]. Zeeman AM, et al. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2858-63.
Animal experiment: | For in vivo PK studies, female CD-1 mice (25 to 30g) are used and randomly assigned to cages. Mice are allowed to acclimate before initiation of the experiments. Feed and water are given ad libitum. KDU691 is formulated at concentrations of 2.5 mg/mL and 0.25 mg/mL for a dose of 25 mg/kg and 2.5 mg/kg, respectively. The suspension formulation for p.o. dosing contains 0.5% Methyl cellulose and 0.5% Tween 80 in water. After oral dosing, blood and liver samples from mice are collected at 0.08 to 24 h post dosing. Groups of three mice are used for each time point. Blood is centrifuged at 13,000 rpm for 7 min at 4°C, plasma harvested and stored at -20°C until analysis. Liver tissue samples are excised, dipped in PBS, gently blotted with absorbent paper, dried, weighed and stored at -20°C until further analysis[1]. |
References: [1]. Zeeman AM, et al. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2858-63. | |
| Cas No. | 1513879-19-0 | SDF | |
| Canonical SMILES | ClC1=CC=C(N(C(C2=CN3C(C=N2)=NC=C3C4=CC=C(C(NC)=O)C=C4)=O)C)C=C1 | ||
| Formula | C22H18ClN5O2 | M.Wt | 419.86 |
| Solubility | DMSO : 150 mg/mL (357.26 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3817 mL | 11.9087 mL | 23.8175 mL |
| 5 mM | 0.4763 mL | 2.3817 mL | 4.7635 mL |
| 10 mM | 0.2382 mL | 1.1909 mL | 2.3817 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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