Antiparasitic agent-30
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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, Ka=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).
For research use only. We do not sell to patients.
- CAS No.: 671754-20-4
- Formula: C19H19N3O2
- Molecular Weight:321.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Parasite Isoforms
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Biological Activity
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Trypanosoma 1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L6 | IC50 |
61.6 μM
Compound: 10
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Cytotoxicity against rat L6 cells
Cytotoxicity against rat L6 cells
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[PMID: 17949068] |
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 (Kd=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.
Chemical Information
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CAS No. 671754-20-4
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Appearance Solid
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Molecular Weight 321.37
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Formula C19H19N3O2
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SMILES
C1(C2=CC=C(OC3=CC=CC=C3)C=C2)=CC(N4CCOCC4)=NN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (270 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)