Q-203 Ditosylate

Alias: Q-203 ditosylate; Q 203 ditosylate; Q203ditosylate

Cat No.:V3784 Purity: ≥98%

COA Product Data Instructions for use SDS

Q203 is an imidazopyridine amide(IAP)compound that block Mycobacterium tuberculosis growth by targeting the respiratory cytochrome bc1 complex.

Q-203 Ditosylate Chemical Structure CAS No.: 1566517-83-6
Product category: Others 5

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Q-203 Ditosylate:

Q203 (IAP6)

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators

Product 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.

Biological Activity I Assay Protocols (From Reference)

ln 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:

ln 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 Protocol

Rats: Sprague Dawley rats are used for pharmacokinetic studies. Compounds (Q203) are given at a dose of 2 mg per kg body weight intravenously or 10 mg per kg body weight orally. The compounds (Q203) are formulated in 20% TPGS (d-α tocopheryl polyethylene glycol 1000 succinate) for repeated-dose studies and in 40% PEG400, pH4 for single-dose studies. Blood samples are taken through the caudal vena cava using 1-mL syringes before perfusion. Samples are collected from three mice or rats at 0.5, 1, 2, 6, 12, 24 and 48 h post-dose. Blood samples are centrifuged at 3,200g for 10 min at 4 °C. Following centrifugation, plasma is collected and frozen until further analysis. Compound concentrations are determined by LC-MS;

Mice: Efficacy of Q203 in a mouse model of established tuberculosis is studied. Bacterial loads are enumerated in the lung of infected mice after 14 d and 28 d of treatment. Q203 is used at 0.4, 2 and 10 mg per kg body weight. Bedaquiline and isoniazid (INH) are used as positive controls at 6.5 and 15 mg per kg body weight, respectively. Five mice per group and per time point are used.

Sprague Dawley rats

References

Nat Med.2013 Sep;19(9):1157-60.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C43H44CLF3N4O8S2

Molecular Weight

901.41

CAS #

1566517-83-6

Related CAS #

1334719-95-7;1566517-83-6 (ditosylate);

SMILES

ClC1C=CC2=NC(CC)=C(C(NCC3C=CC(=CC=3)N3CCC(C4C=CC(=CC=4)OC(F)(F)F)CC3)=O)N2C=1.S(C1C=CC(C)=CC=1)(=O)(=O)O.S(C1C=CC(C)=CC=1)(=O)(=O)O

Synonyms

Q-203 ditosylate; Q 203 ditosylate; Q203ditosylate

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: >10 mM

Water:N/A

Ethanol:N/A

Solubility (In Vivo)

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. O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.1094 mL	5.5469 mL	11.0937 mL
	5 mM	0.2219 mL	1.1094 mL	2.2187 mL
	10 mM	0.1109 mL	0.5547 mL	1.1094 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

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Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (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.