2. Anti-infection
  3. Parasite Bacterial Antibiotic
  4. SQ109

SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC50 for cell killing of 50±8 nM. SQ109, targets MmpL3, is an antitubercular agent.

For research use only. We do not sell to patients.

SQ109 Chemical Structure

SQ109 Chemical Structure

CAS No. : 502487-67-4

Size Price Stock Quantity
5 mg USD 175 In-stock
10 mg USD 280 In-stock
25 mg USD 588 In-stock
50 mg USD 940 In-stock
100 mg USD 1500 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

SQ109 Related Antibodies

Top Publications Citing Use of Products

View All Parasite Isoform Specific Products:

View All Isoforms
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

View All Antibiotic Isoform Specific Products:

View All Isoforms
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC50 for cell killing of 50±8 nM. SQ109, targets MmpL3, is an antitubercular agent.

IC50 & Target

Trypanosoma

 

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
18 μM
Compound: 1, SQ109
Cytotoxicity against human MCF7 cells assessed as growth inhibition by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition by MTT assay
[PMID: 24568559]
In Vitro

SQ109 also inhibits extracellular epimastigotes (IC50, 4.6±1 μM) and the clinically relevant intracellular amastigotes (IC50, ~0.5 to 1 μM), with a selectivity index of ~10 to 20. SQ109 has little effect (EC50, ~80 μM) in a red blood cell hemolysis assay. Besides, SQ109 causes major ultrastructural changes in all three life cycle forms, as observed by light microscopy, scanning electron microscopy (SEM), and transmission electron microscopy (TEM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SQ109 Related Antibodies
In Vivo

Oral administration of SQ109 (0.1-25 mg/kg per day) to the mice for 28 days results in dose-dependent reductions of mycobacterial load in both spleen and lung comparable to that of EMB administered at 100 mg/kg per day, but is less potent than isoniazid (INH) at 25 mg/kg per day. Pharmacokinetic profiles of SQ109 in mice following a single administration showed its Cmax as 1038 (intravenous (i.v.)) and 135 ng/mL (p.o.), with an oral Tmax of 0.31 h. The elimination t1/2 of SQ109 is 3.5 (i.v.) and 5.2 h (p.o.). The oral bioavailability is 4%[2]. The terminal half-life (t1/2) of SQ109 in dogs (12-29 h, mean 29.3 h) is longer than in rats (7-8 h, mean 7.4 h), as reflected by the significantly larger volume of distribution of SQ109 in dogs. The oral bioavailability of SQ109 in rats and dogs is determined to be 12% and 5%, respectively[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

330.55

Formula

C22H38N2
CAS No.
Appearance

Liquid (Density: 0.97±0.1 g/cm3)

Color

Light yellow to yellow

SMILES

C/C(C)=C/CC/C(C)=C/CNCCNC1[C@H]2C[C@H]3C[C@@H]1C[C@H](C3)C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (75.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0253 mL 15.1263 mL 30.2526 mL
5 mM 0.6051 mL 3.0253 mL 6.0505 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.24%

SDS (393 KB)

COA (242 KB) HNMR (259 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

The LLC-MK2 cells are treated with SQ109 (2.5 to 20 μM) and incubated for 96 h at 37°C. Fresh RPMI 1640 medium containing only 10% FBS is added to the untreated samples as a control. To determine toxicity, the MTS/PMS assay is performed. The selectivity index of SQ109 is determined based on its activities against the trypomastigote and intracellular amastigote forms of T.cruzi, calculated as the ratio of the 50% cytotoxic concentration (CC50) of mammalian cells to the IC50 or 50% lysing concentration (LC50) of T.cruzi. All experiments are performed in duplicate. The means are determined from ≥3 experiments[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Mice[2]
Female C57BL/6 mice (8 weeks old) are used. Oral treatment of mice with INH (25 mg/kg), ethambutol (EMB) (100 mg/kg) and SQ109 (0.1, 10 and 25 mg/kg) is initiated 20 days after inoculation. Control groups of infected but untreated mice are killed at the initiation of therapy (early controls) or at the end of the treatment period. There are six mice per group. Chemotherapy is given daily for 5 days per week until the mice are killed, 4 weeks after initiation of treatment. The spleen and lungs are aseptically removed and weighed. The organs are homogenized in 2 ml of sterile PBS containing 0.05% Tween-80. Homogenate samples from individual tissues are diluted 10-fold in PBS and plated on 7H10 agar dishes. Inoculated dishes are incubated at 37°C in ambient air for 3 weeks prior to calculation of CFU. Viable counts are converted to a logarithmic scale; readings are corrected to represent whole organ totals. The severity of infection and the effectiveness of the treatments are assessed by the survival rate, and the mean number of CFU in mouse organs.
Rats and Dogs[3]
Male Fischer rats (271-289 g) and beagle dogs (7.5-8.9 kg, two males and two females per dose group) are used. Rats are given either a single intravenous (i.v.) bolus dose of 1.5 mg/kg (9 mg/m2) or an oral dose of 13 mg/kg (78 mg/m2) of SQ109 (n=8 per dose group); rats are divided into subgroups consisting of four rats per subgroup. Rat blood (0.7 mL) is withdrawn from the jugular vein catheter at alternating time points from individual rats in each subgroup. Blood samples are collected at 2, 5, 10, 15 and 30 min and 1, 3, 6, 10 and 24 h after a single i.v. administration, or 5, 15 and 30 min and 1, 2, 4, 6, 10 and 24 h after a single oral administration. Each blood sample is centrifuged to separate plasma, which is then stored at −70°C until analysis. Beagle dogs are dosed by gavage at either 3.75 or 15 mg/kg (75 or 300 mg/m2), or intravenously at either 0.45 or 4.5 mg/kg (9 and 90 mg/m2). Dog blood (0.7 mL) is withdrawn from the jugular vein at 2, 5, 10, 20 and 30 min and 1, 2, 4, 8, 12, 18 and 24 h after a single i.v. administration, or 10, 20 and 30 min and 1, 2, 4, 8, 12, 18 and 24 h after a single oral administration.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 3.0253 mL 15.1263 mL 30.2526 mL 75.6315 mL
5 mM 0.6051 mL 3.0253 mL 6.0505 mL 15.1263 mL
10 mM 0.3025 mL 1.5126 mL 3.0253 mL 7.5632 mL
15 mM 0.2017 mL 1.0084 mL 2.0168 mL 5.0421 mL
20 mM 0.1513 mL 0.7563 mL 1.5126 mL 3.7816 mL
25 mM 0.1210 mL 0.6051 mL 1.2101 mL 3.0253 mL
30 mM 0.1008 mL 0.5042 mL 1.0084 mL 2.5211 mL
40 mM 0.0756 mL 0.3782 mL 0.7563 mL 1.8908 mL
50 mM 0.0605 mL 0.3025 mL 0.6051 mL 1.5126 mL
60 mM 0.0504 mL 0.2521 mL 0.5042 mL 1.2605 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

SQ109 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SQ109502487-67-4NSC 722041SQ 109SQ-109NSC722041NSC-722041ParasiteBacterialAntibioticInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SQ109
Cat. No.:
HY-14989
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.