SQ641
SQ641 is a translocase I (TL1) inhibitor that blocks peptidoglycan biosynthesis. SQ641 exerts bactericidal activity against Mycobacterium tuberculosis and has a prolonged post-antibiotic effect. SQ641 shows synergistic activity with Ethambutol (HY-B0535), Streptomycin (HY-B1906), and SQ109 (HY-14989), and is able to suppress the emergence of drug-resistant mycobacterial mutants. SQ641-derived phospholipid-based nanoemulsion formulation SQ641-NE exhibits intracellular activity against Mycobacterium tuberculosis in macrophages and reduces splenic CFU in mouse tuberculosis models. SQ641 in TPGS-solubilized solutions or TPGS micelles reduces lung CFU. SQ641 can be used for research on tuberculosis.
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- CAS No.: 254449-23-5
- Formule: C34H51N5O13
- Masse moléculaire:737.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
SQ641 exhibits activity against M. tuberculosis (MIC 1.0 µg/mL) and the M. avium complex (MIC 0.016-16 µg/mL), with a post-antibiotic effect against M. tuberculosis of 55 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SQ641-derived phospholipid-based nanoemulsion formulation SQ641-NE (100-250 mg/kg; i.v. twice weekly for 4 weeks; i.p. five times weekly for 4 weeks) shows reduced efficacy in M. tuberculosis-infected C57BL/6 mice, with only a modest reduction in spleen CFU and no reduction in lung CFU[1].
SQ641 (25-100 mg/kg; i.p. or i.v.; five times per week or twice per week; 4 weeks) reduces M. tuberculosis CFU in the lungs of chronically infected mice, where i.v. micelle monotherapy at 50 mg/kg produces the lowest lung CFU, and the i.v. combination with INH (HY-B0329) further reduces CFU[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, were infected intravenously with 105 CFU H37Rv, and therapy was initiated 3 weeks later)[1]
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Dosage:100 mg/kg
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Administration:i.v. twice weekly for 4 weeks (8 doses)
i.p. five times weekly for 4 weeks -
Result:Produced modest CFU reductions in spleen and lungs of M. tuberculosis-infected C57BL/6 mice, with greater splenic activity and bacteriostasis in lungs.
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Animal Model:C57BL/6 (female, were infected intravenously with 105 CFU H37Rv, and therapy was initiated 3 weeks later)[1]
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Dosage:100 mg/kg (i.v.)
250 mg/kg (i.p.) -
Administration:i.v. twice weekly for 4 weeks
i.p. five times weekly for 4 weeks -
Result:Reduced spleen CFU to 6.02 log10 (0.47 log10 reduction) and lung CFU to 6.67 log10 (0.09 log10 reduction) at 100 mg/kg by intravenous administration.
Lowered spleen CFU to 5.94 log10 (0.55 log10 reduction) and lung CFU to 6.91 log10 (0.15 log10 increase) at 250 mg/kg via intraperitoneal injection.
Maintained bacteriostatic effects within the lungs.
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Animal Model:C57BL/6 (female, were infected intravenously with M. tuberculosis H37Rv, and therapy was initiated 3 weeks later)[2]
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Dosage:50 mg/kg (TPGS solution, i.p.); 25 mg/kg (TPGS solution, i.v.); 100 mg/kg (TPGS micelles, i.p.); 50 mg/kg (TPGS micelles, i.v.); 25 mg/kg (TPGS solution, i.v. + INH); 25 mg/kg (micelles, i.v. + INH)
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Administration:i.p., five times/week for 4 weeks
i.v., two times/week for 4 weeks -
Result:Reduced lung log10 CFU to 6.70 for TPGS‑formulated SQ641 at 50 mg/kg via intraperitoneal administration.
Reduced lung log10 CFU to 6.10 for TPGS‑formulated SQ641 at 25 mg/kg via intravenous administration.
Reduced lung log10 CFU to 6.15 for TPGS‑micelle‑encapsulated SQ641 at 100 mg/kg via intraperitoneal administration.
Reduced lung log10 CFU to 6.01 for TPGS‑micelle‑encapsulated SQ641 at 50 mg/kg via intravenous administration.
Decreased lung CFU by 2.08 log10.
Reduced lung log10 CFU to 4.64 for combined treatment of TPGS‑formulated SQ641 (25 mg/kg, i.v.) plus INH.
Reduced lung log10 CFU to 4.46 for combined treatment of micelle‑encapsulated SQ641 (25 mg/kg, i.v.) plus INH.
Chemical Information
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CAS No. 254449-23-5
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Masse moléculaire 737.80
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Formule C34H51N5O13
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SMILES
O(C(CCCCCCCCC)=O)[C@H]1[C@@H](O[C@]([C@@H](O[C@H]2OC(C(N[C@@H]3C(=O)N[C@H](C)CCC3)=O)=C[C@H](O)[C@@H]2O)C(N)=O)([C@H]1OC)[H])N4C(=O)NC(=O)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SQ641 Related Classifications
HY-187919 Related Classifications
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