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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 254449-23-5
- 分子式: C34H51N5O13
- 分子量:737.80
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保管条件:
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 254449-23-5
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分子量 737.80
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
SQ641 関連分類
HY-187919 関連分類
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