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100mg | $1050 | Check With Us |
200mg | $1575 | Check With Us |
500mg | $2650 | Check With Us |
Cat #: V3011 CAS #: 1334719-95-7 Purity ≥ 98%
Description: Q203 is an imidazopyridine amide (IAP) compound that block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. It has the potential for the treatment of tuberculosis. Q203 inhibited the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight, which highlights the potency of Q203. Q203 is active against the reference strain Mycobacterium tuberculosis H37Rv with MIC50s of 2.7 nM in culture broth medium and 0.28 nM inside macrophages. In addition, Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Together, these data indicate that Q203 is a promising new clinical candidate for the treatment of tuberculosis.
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Molecular Weight (MW) | 557.01 |
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Molecular Formula | C29H28ClF3N4O2 |
CAS No. | 1334719-95-7 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 10 mMr |
Water: <1 mg/mLr | |
Ethanol: <1 mg/mL | |
SMILES Code | O=C(C1=C(CC)N=C2C=CC(Cl)=CN21)NCC3=CC=C(N4CCC(C5=CC=C(OC(F)(F)F)C=C5)CC4)C=C3 |
Synonyms | Q-203; Q 203; Q203 |
Protocol | In Vitro | In vitro activity: Q203 is an imidazopyridine amide (IAP) compound that block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. It has the potential for the treatment of tuberculosis. Q203 inhibited the growth of MDR and XDR M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight, which highlights the potency of Q203. Q203 is active against the reference strain Mycobacterium tuberculosis H37Rv with MIC50s of 2.7 nM in culture broth medium and 0.28 nM inside macrophages. In addition, Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Together, these data indicate that Q203 is a promising new clinical candidate for the treatment of tuberculosis. Kinase Assay: Q203 is active against the reference strain Mycobacterium tuberculosis H37Rv with MIC50s of 2.7 nM in culture broth medium and 0.28 nM inside macrophages. Cell Assay: |
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In Vivo | Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Q203 has a bioavailability of 90% and a terminal half-life of 23.4 h. The volume of distribution is moderate (5.27 l per kg body weight), and the systemic clearance is low (4.03 mL/min per kg). After 4 weeks of treatment, reductions of 90%, 99% and 99.9% in M. tuberculosis H37Rv bacterial load is observed in the groups treated with Q203 at 0.4, 2 and 10 mg per kg body weight, respectively | |
Animal model | Sprague Dawley rats |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7953 mL | 8.9765 mL | 17.9530 mL | 35.9060 mL |
5mM | 0.3591 mL | 1.7953 mL | 3.5906 mL | 7.1812 mL |
10mM | 0.1795 mL | 0.8976 mL | 1.7953 mL | 3.5906 mL |
20mM | 0.0898 mL | 0.4488 mL | 0.8976 mL | 1.7953 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.