Antiparasitic agent-30 

Antiparasitic agent-30 is a potent adenosine kinase TbrAK modulator and antitrypanosomal agent. Antiparasitic agent-30 exhibits significant inhibitory activity against Trypanosoma brucei rhodesiense, while enhancing the activity of recombinant TbrAK(EC₅₀=38 nM, K_a=75 nM-497 nM). Antiparasitic agent-30 exerts its pharmacological effects by eliminating intrinsic substrate inhibition and hyperactivating TbrAK in Trypanosoma brucei rhodesiense. Antiparasitic agent-30 serves as a valuable tool molecule for studying acute African human trypanosomiasis (sleeping sickness)^[1].

Antiparasitic agent-30 (Compound 1) potently inhibits the viability of T. b. rhodesiense parasites, with an IC₅₀ of 1.0 μM^[1].
Antiparasitic agent-30 (1-750 μM; 10 min) enhances the activity of recombinant TbrAK in a concentration-dependent manner, with an EC₅₀ of 38.9 μM, and increases the activity by 2.5-fold at 50 μM^[1].
Antiparasitic agent-30 enhances the activity of recombinant TbrAK in radiometric assays, with a highly potent EC₅₀ of 38 nM^[1].
Antiparasitic agent-30 (150 μM) binds to two distinct sites of recombinant TbrAK (7 μM), and exhibits high affinity for the primary binding site (K_d=75 nM)^[1].
Antiparasitic agent-30 exhibits reduced potency against T. b. brucei parasites with silenced TbAK, with its IC₅₀ increasing from 131 nM to 271 nM, confirming that its activity depends on the expression of adenosine kinase^[1].

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

321.37

C₁₉H₁₉N₃O₂

671754-20-4

Solid

C1(C2=CC=C(OC3=CC=CC=C3)C=C2)=CC(N4CCOCC4)=NN1

Room temperature in continental US; may vary elsewhere.

• [1]. Kuettel S, et al. Adenosine Kinase of T. b. rhodesiense identified as the putative target of 4-[5-(4-phenoxyphenyl)-2 H-pyrazol-3-yl] morpholine using chemical proteomics[J]. PLoS neglected tropical diseases, 2009, 3(8): e506.