IID432
Based on 1 Customer Validation
IID432 is a potent, orally active, and covalent inhibitor of Trypanosoma cruzi topoisomerase II. IID432 shows an EC50 of 8 nM against T. cruzi intracellular amastigotes, exhibits excellent oral bioavailability (52% in rats), favorable ADME properties, and no S1P pathway modulation. IID432 achieves relapse-free cure in a chronic T. cruzi infection mouse model, can be used for the study of Chagas disease.
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- CAS No.: 3094992-69-2
- 화학식: C19H19N7O
- 분자량:361.40
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Topoisomerase II |
IID432 (6 days) inhibits the growth of intracellular T. cruzi amastigotes in T. cruzi-infected NIH 3T3 fibroblasts with an EC50 of 8 nM[1].
IID432 (4 days) displays no cytotoxicity toward NIH 3T3 fibroblasts (CC50 > 20 μM)[1].
IID432 exhibits decreased potency against CRISPR-generated topoisomerase II mutant strains of T. brucei (>150-fold) relative to wild-type parasites[1].
IID432 (10 μM; 24 h) does not significantly increase intracellular sphingosine-1-phosphate (S1P) levels in HEK293T cells (1.2-fold increase) compared to DMSO control[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T. cruzi-infected NIH 3T3 fibroblasts
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Concentration:1 nM-20 μM
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Incubation Time:6 days
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Result:Showed an EC50 of 8 nM.
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Cell Line:NIH 3T3 fibroblasts
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Concentration:1 nM-20 μM
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Incubation Time:4 days
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Result:Displayed no cytotoxicity toward NIH 3T3 fibroblasts (CC50 > 20 μM).
IID432 (25 mg/kg; p.o.; single dose) fully eliminates parasites in all treated animals in a chronic T. cruzi infection model in BALB/c mice (~100 days post-infection), with no detectable parasites after cyclophosphamide-induced immunosuppression (3 rounds at days 112, 116, and 120 post-treatment)[1].
IID432 (30 mg/kg/day; p.o.; once daily for 14 days) does not trigger S1P accumulation in the kidney or spleen relative to vehicle in Wistar rats, and maintains hematological parameters within the normal range[1].
IID432 (up to 50 mg/kg/day; p.o.; once daily for 14 days) is well tolerated in nonhuman primates with no significant adverse effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic T. cruzi infection model in BALB/c mice[1]
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Dosage:5 mg/kg
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Administration:p.o.; once daily for 3 days
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Result:Showed incomplete parasite clearance.
Could not prevent parasite reappearance after cyclophosphamide-induced immunosuppression
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Animal Model:Chronic T. cruzi infection model in BALB/c mice[1]
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Dosage:10 mg/kg
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Administration:p.o.; once daily for 3 days
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Result:Achieved sterile cure with no relapse after cyclophosphamide immunosuppression.
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Animal Model:Chronic T. cruzi infection model in BALB/c mice[1]
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Dosage:25 mg/kg
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Administration:p.o.; single dose
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Result:Eliminated parasites in all treated animals.
Showed no parasite signal after cyclophosphamide-induced immunosuppression.
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Animal Model:Safety study in Wistar rats[1]
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Dosage:30 mg/kg/day
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Administration:p.o.; once daily for 14 days
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Result:Did not trigger S1P accumulation in the kidney or spleen relative to vehicle.
Maintained hematological parameters within the normal range.
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Animal Model:Safety study in nonhuman primates[1]
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Dosage:Up to 50 mg/kg/day
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Administration:p.o.; once daily for 14 days
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Result:Showed well tolerance in nonhuman primates with no significant adverse effects.
Chemical Information
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CAS No. 3094992-69-2
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Appearance Solid
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분자량 361.40
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화학식 C19H19N7O
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Color Light yellow to brown
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SMILES
CC1=NC2=C(C=C(C=C2)N3CC[C@@H](C3)NC(CN4C=NC(C#N)=N4)=O)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (138.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (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
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 | 2.7670 mL | 13.8351 mL | 27.6702 mL | 69.1754 mL |
| 5 mM | 0.5534 mL | 2.7670 mL | 5.5340 mL | 13.8351 mL | |
| 10 mM | 0.2767 mL | 1.3835 mL | 2.7670 mL | 6.9175 mL | |
| 15 mM | 0.1845 mL | 0.9223 mL | 1.8447 mL | 4.6117 mL | |
| 20 mM | 0.1384 mL | 0.6918 mL | 1.3835 mL | 3.4588 mL | |
| 25 mM | 0.1107 mL | 0.5534 mL | 1.1068 mL | 2.7670 mL | |
| 30 mM | 0.0922 mL | 0.4612 mL | 0.9223 mL | 2.3058 mL | |
| 40 mM | 0.0692 mL | 0.3459 mL | 0.6918 mL | 1.7294 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5534 mL | 1.3835 mL | |
| 60 mM | 0.0461 mL | 0.2306 mL | 0.4612 mL | 1.1529 mL | |
| 80 mM | 0.0346 mL | 0.1729 mL | 0.3459 mL | 0.8647 mL | |
| 100 mM | 0.0277 mL | 0.1384 mL | 0.2767 mL | 0.6918 mL |
IID432 Related Classifications
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