Product Name :
UCT943
Description:
UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.
CAS:
1450666-80-4
Molecular Weight:
427.42
Formula:
C22H20F3N5O
Chemical Name:
5-[4-(piperazine-1-carbonyl)phenyl]-3-[4-(trifluoromethyl)phenyl]pyrazin-2-amine
Smiles :
NC1=NC=C(N=C1C1C=CC(=CC=1)C(F)(F)F)C1C=CC(=CC=1)C(=O)N1CCNCC1
InChiKey:
GGOFGCMPKAWHEZ-UHFFFAOYSA-N
InChi :
InChI=1S/C22H20F3N5O/c23-22(24,25)17-7-5-15(6-8-17)19-20(26)28-13-18(29-19)14-1-3-16(4-2-14)21(31)30-11-9-27-10-12-30/h1-8,13,27H,9-12H2,(H2,26,28)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Mucicarmine} MedChemExpress|{Mucicarmine} {Fluorescent Dye}|{Mucicarmine} Protocol|{Mucicarmine} In Vivo|{Mucicarmine} manufacturer|{Mucicarmine} Autophagy}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.|Product information|CAS Number: 1450666-80-4|Molecular Weight: 427.42|Formula: C22H20F3N5O|Chemical Name: 5-[4-(piperazine-1-carbonyl)phenyl]-3-[4-(trifluoromethyl)phenyl]pyrazin-2-amine|Smiles: NC1=NC=C(N=C1C1C=CC(=CC=1)C(F)(F)F)C1C=CC(=CC=1)C(=O)N1CCNCC1|InChiKey: GGOFGCMPKAWHEZ-UHFFFAOYSA-N|InChi: InChI=1S/C22H20F3N5O/c23-22(24,25)17-7-5-15(6-8-17)19-20(26)28-13-18(29-19)14-1-3-16(4-2-14)21(31)30-11-9-27-10-12-30/h1-8,13,27H,9-12H2,(H2,26,28)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (584.{{Anti-Mouse TNFR2 Antibody} medchemexpress|{Anti-Mouse TNFR2 Antibody} Apoptosis|{Anti-Mouse TNFR2 Antibody} Purity & Documentation|{Anti-Mouse TNFR2 Antibody} In Vivo|{Anti-Mouse TNFR2 Antibody} manufacturer|{Anti-Mouse TNFR2 Antibody} Autophagy} 90 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|UCT943 maintains high in vitro selectivity (>200-fold) for the parasite PvPI4K versus the human PI4Kβ isozyme (IC50 of PI4Kβ, 5.PMID:23443926 4 μM), inhibition of which is linked to immunosuppressive effects. 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.|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.|Products are for research use only. Not for human use.|
