1. Anti-infection
  2. Parasite
    Bacterial
  3. SQ109

SQ109 (Synonyms: NSC 722041)

Cat. No.: HY-14989 Purity: >98.0%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 377 In-stock
Estimated Time of Arrival: December 31
5 mg USD 343 In-stock
Estimated Time of Arrival: December 31
10 mg USD 443 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1195 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE SQ109

  • 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

IC50: 50±8 nM (trypomastigote cell)[1]

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].

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].

Molecular Weight

330.55

Formula

C₂₂H₃₈N₂

CAS No.

502487-67-4

SMILES

C/C(C)=C/CC/C(C)=C/CNCCNC1[[email protected]]2C[[email protected]]3C[[email protected]@H]1C[[email protected]](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)

*"≥" 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
10 mM 0.3025 mL 1.5126 mL 3.0253 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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
  • 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.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SQ109
Cat. No.:
HY-14989
Quantity: