2. PI3K/Akt/mTOR Anti-infection
  3. PI4K Parasite
  4. UCT943

UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.

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UCT943 Chemical Structure

UCT943 Chemical Structure

CAS No. : 1450666-80-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 605 In-stock
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10 mM * 1 mL in DMSO USD 605 In-stock
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10 mg USD 950 In-stock
50 mg USD 2950 In-stock
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Based on 1 publication(s) in Google Scholar

UCT943 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM[1].

IC50 & Target[1]

PvPI4K

23 nM (IC50)

Plasmodium

 

In Vitro

UCT943 maintains high in vitro selectivity (>200-fold) for the parasite PvPI4K versus the human PI4Kβ isozyme (IC50 of PI4Kβ, 5.4 μM), inhibition of which is linked to immunosuppressive effects[1].
In vitro cytotoxicity of UCT943 is tested against L6 cells, chinese hamster ovarian (CHO), Vero, and HepG2 cells, with 50% cytotoxic concentrations (CC50s) of 12, 17, 113, and 13 μM, respectively[1].

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

UCT943 Related Antibodies
In Vivo

UCT943 shows excellent in vivo efficacy in the Plasmodium berghei (10 mg/kg and 3 mg/kg; oral administration; daily; 4 days) and P. falciparum NSG (NOD-scid IL-2Rγnull) mouse models (0.01, 0.1, 0.3, 1.1 and 10 mg/kg; oral administration; once per day; 4 days). When dosed at 10 mg/kg per os (p.o.), UCT943 reduces parasitemia by >99.9% in the mouse P. berghei infection model and cures all mice, with >30 mean survival days (MSD). At 3 mg/kg p.o., no complete cure is achieved, and MSD is 10 days, albeit parasitemia is reduced by 99%. The resulting 90% effective dose (ED90) is 1.0 mg/kg p.o. in the P. berghei infection model. The ED90 is 0.25 mg/kg in the P. falciparum-infected NSG mouse model[1].

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

Animal Model: Mice with P. berghei and P. falciparum NOD-scid IL-2Rγnull (NSG) models[1]
Dosage: 10 mg/kg and 3 mg/kg for P. berghei model; 0.01, 0.1, 0.3, 1.1 and 10 mg/kg for P. falciparum NOD-scid IL-2Rγnull (NSG) model
Administration: Oral administration; daily; 4 days for P. berghei model
Oral administration; once per day; 4 days for P. falciparum NOD-scid IL-2Rγnull (NSG) model
Result: The ED90 is 1.0 mg/kg in the P. berghei infection model. The ED90 is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.
Molecular Weight

427.42

Formula

C22H20F3N5O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(F)(F)C1=CC=C(C2=NC(C3=CC=C(C(N4CCNCC4)=O)C=C3)=CN=C2N)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (584.90 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 2.3396 mL 11.6981 mL 23.3962 mL
5 mM 0.4679 mL 2.3396 mL 4.6792 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.08 mg/mL (4.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3396 mL 11.6981 mL 23.3962 mL 58.4905 mL
5 mM 0.4679 mL 2.3396 mL 4.6792 mL 11.6981 mL
10 mM 0.2340 mL 1.1698 mL 2.3396 mL 5.8490 mL
15 mM 0.1560 mL 0.7799 mL 1.5597 mL 3.8994 mL
20 mM 0.1170 mL 0.5849 mL 1.1698 mL 2.9245 mL
25 mM 0.0936 mL 0.4679 mL 0.9358 mL 2.3396 mL
30 mM 0.0780 mL 0.3899 mL 0.7799 mL 1.9497 mL
40 mM 0.0585 mL 0.2925 mL 0.5849 mL 1.4623 mL
50 mM 0.0468 mL 0.2340 mL 0.4679 mL 1.1698 mL
60 mM 0.0390 mL 0.1950 mL 0.3899 mL 0.9748 mL
80 mM 0.0292 mL 0.1462 mL 0.2925 mL 0.7311 mL
100 mM 0.0234 mL 0.1170 mL 0.2340 mL 0.5849 mL
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UCT943 Related Classifications

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:

UCT9431450666-80-4UCT 943UCT-943PI4KParasitePhosphatidylinositol 4 kinasesPI4 kinasesInhibitorinhibitorinhibit

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