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SQ109

Catalog No. T16925 CAS 502487-67-4

Synonyms: NSC 722041

SQ109 (NSC-722041) is an effective inhibitor of the trypomastigote form of the parasite (IC50 = 50 nM). SQ109 is an antitubercular agent and targets MmpL3.

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SQ109, CAS 502487-67-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 60.00
5 mg	In stock	$ 143.00
10 mg	In stock	$ 228.00
25 mg	In stock	$ 487.00
50 mg	In stock	$ 713.00
100 mg	In stock	$ 987.00
500 mg	In stock	$ 1,980.00
1 mL * 10 mM (in DMSO)	In stock	$ 159.00

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Purity: 99.3%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SQ109 (NSC-722041) is an effective inhibitor of the trypomastigote form of the parasite (IC50 = 50 nM). SQ109 is an antitubercular agent and targets MmpL3.
Targets&IC50	Parasite:50 nM(trypomastigote cell)
In vitro	SQ109 causes major ultrastructural changes in all three life cycle forms. SQ109 inhibits extracellular epimastigotes (IC50 = 4.6μM) and the clinically relevant intracellular amastigotes (IC50 = 0.5 - 1 μM), with a selectivity index of 10 to 20. SQ109 has little effect (EC50 = 80 μM) in a red blood cell hemolysis assay[1].
In vivo	The 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 12% and 5%, respectively[2]. SQ109 (0.1-25 mg/kg) to the mice for 28 days results in dose-dependent reductions of mycobacterial load in both spleen and lung comparable to that of EMB(100 mg/kg), but is less potent than isoniazid(25 mg/kg). Pharmacokinetic profiles of SQ109 in mice following a single administration showed its Cmax as 1038 (i.v.) and 135 ng/mL (p.o.), with an oral Tmax of 0.31 h and an oral bioavailability of 4%. The elimination t1/2 of SQ109 is 3.5 (i.v.) and 5.2 h (p.o.)[3].

Synonyms	NSC 722041
Molecular Weight	330.55
Formula	C22H38N2
CAS No.	502487-67-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (75.63 mM)

References and Literature

1. Veiga-Santos P, et al. SQ109, a new drug lead for Chagas disease. Antimicrob Agents Chemother. 2015 Apr;59(4):1950-61. 2. Jia L, et al. Pharmacodynamics and pharmacokinetics of SQ109, a new diamine-based antitubercular drug. Br J Pharmacol. 2005 Jan;144(1):80-7 3. Jia L, et al. Interspecies pharmacokinetics and in vitro metabolism of SQ109. Br J Pharmacol. 2006 Mar;147(5):476-85.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Anti-Parasitic Compound Library ReFRAME Related Library Clinical Compound Library Orally Active Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SQ109 502487-67-4 Microbiology/Virology Others Parasite SQ 109 NSC-722041 NSC722041 Bacterial Inhibitor inhibit NSC 722041 Antibiotic SQ-109 inhibitor

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