SQ109, inhibitor

SQ109

Cat. Num. AAA5755550

• Purity: 98.00%
• Synonyms: SQ109; NSC 722041; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 25mg/mL (75.63mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C22H38N2
• SMILES: C/C(C)=C/CC/C(C)=C/CNCCNC1[C@H]2C[C@H]3C[C@@H]1C[C@H](C3)C2
• CAS Number: 502487-67-4
• Target & IC50: trypomastigote cell: ic50 50+/-8nM
• In Vitro: SQ109 (0.1-25mg/kg per day, p.o., mice for 28 days) causes dose-dependent reductions of mycobacterial load in both spleen and lung comparable to that of EMB administered at 100mg/kg per day but is less potent than isoniazid at 25mg/kg per day. Pharmacokinetic profiles of SQ109 in mice following a single administration showed its Cmax as 1038 (i.v.) and 135ng/mL (p.o.), with an oral Tmax of 0.31 hours. The elimination t1/2 of SQ109 is 3.5 (i.v.) and 5.2 h (p.o.). The oral bioavailability is 4%. The terminal half-life (t1/2) of SQ109 in dogs (12-29 hours, mean 29.3 hours) 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 [2][3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for SQ109, inhibitor

SQ109 is an effective inhibitor of the trypomastigote form of the parasite (IC50 for cell killing: 50+/-8nM). SQ109 is an antitubercular agent.

References

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