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Q203

Cat. No. M5297
Q203 Structure
Synonym:

Q-203; Q 203; IAP6

Size Price Availability Quantity
10mM*1mL In DMSO USD 450 In stock
2mg USD 244 In stock
5mg USD 375 In stock
10mg USD 556 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: Imidazopyridine amide (IPA) compounds block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex. The optimized IPA compound Q203 inhibits the growth of MDR and XDR Mycobacterium tuberculosis clinical isolates in culture broth medium in the low nanomolar range. 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 vivo: Q203 is efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight. 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.

Customer Product Validations & Biological Datas
Source Sci Rep (2018). Figure 3. Q203
Method Oxygen consumption activity assay
Cell Lines M. tuberculosis strain
Concentrations 10 μM
Incubation Time -
Results However, inhibition of respiratory chain activity by Q203 was incomplete, with ~60% inhibition observed at the highest Q203 concentration tested (10 μM)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 557.01
Formula C29H28ClF3N4O2
CAS Number 1334719-95-7
Purity >98%
Solubility 10mM in DMSO
Storage at -20°C
References

Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.
Kang S, et al. J Med Chem. 2014 Jun 26;57(12):5293-305. PMID: 24870926.

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis.
Pethe K, et al. Nat Med. 2013 Sep;19(9):1157-60. PMID: 23913123.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Q203, Q-203; Q 203; IAP6 supplier, Anti-infection, inhibitors

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