UCT943
UCT943 Basic information
- Product Name:
- UCT943
- Synonyms:
-
- UCT943
- Methanone, [4-[5-amino-6-[4-(trifluoromethyl)phenyl]-2-pyrazinyl]phenyl]-1-piperazinyl-
- UCT-943,UCT943
- UCT943, 10 mM in DMSO
- (4-(5-amino-6-(4-(trifluoromethyl)phenyl)pyrazin-2-yl)phenyl)(piperazin-1-yl)methanone
- CAS:
- 1450666-80-4
- MF:
- C22H20F3N5O
- MW:
- 427.42
- Mol File:
- 1450666-80-4.mol
UCT943 Chemical Properties
- Boiling point:
- 568.7±50.0 °C(Predicted)
- Density
- 1.321±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 250 mg/mL (584.90 mM; Need ultrasonic)
- form
- Solid
- pka
- 8.25±0.10(Predicted)
- color
- Light yellow to yellow
UCT943 Usage And Synthesis
Uses
UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM[1].
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. bergheiinfection 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. bergheiinfection model. The ED90 is 0.25 mg/kg in the P. falciparum-infected NSG mouse model[1].
| 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. |
IC 50
PvPI4K: 23 nM (IC50); Plasmodium
References
[1] Brunschwig C, et al. UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria. Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. DOI:10.1128/AAC.00012-18
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