HT-61

• CAS: 936622-80-9
• Catalog Number: ACM936622809
• Category: Others
• Molecular Weight: 380.49
• Molecular Formula: C26H24N2O
• Description: HT-61, also known as HY-50A, is a pyrroloquinolone antibiotic potentially for the treatment of staphylococcal infections. HT61 was effective at reducing biofilm viability and was associated with increased expression of cell wall stress and division proteins, confirming its potential as a treatment for S. aureus biofilm infections. HT61 enhances the effect of tobramycin against Pseudomonas aeruginosa in vitro and in vivo.
• Synonyms: HT-61; HT61; HT 61; HY-50A; HY 50A; HY50A
• IUPAC Name: 4-methyl-1-phenethyl-8-phenoxy-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline
• Canonical SMILES: CC1=NC2=CC=C(OC3=CC=CC=C3)C=C2C4=C1CCN4CCC5=CC=CC=C5
• InChI: InChI=1S/C26H24N2O/c1-19-23-15-17-28(16-14-20-8-4-2-5-9-20)26(23)24-18-22(12-13-25(24)27-19)29-21-10-6-3-7-11-21/h2-13,18H,14-17H2,1H3
• InChI Key: XCZMUTGHJBFKPM-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: HT-61, also known as HY-50A, is a pyrroloquinolone antibiotic potentially for the treatment of staphylococcal infections.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 82.07; H, 6.36; N, 7.36; O, 4.20
• Exact Mass: 380.1889
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: The cellular response of planktonic and biofilm cultures following treatment with 0, 4, or 16 mg/liter HT61 was then investigated using ultraperformance liquid chromatography-mass spectrometryElevated Energy (UPLC/MSE). Treatment of planktonic cultures with a sub-MIC concentration of HT61 (4 mg/liter) revealed upregulation of MurD and MurI, two cell wall biosynthesis-associated proteins required for the incorporation of d-glutamate into cell wall peptidoglycans. Increasing the concentration of HT61 from 4 mg/liter to 16 mg/liter led to upregulation of 93% (14/15) of the proteins associated with cell wall biosynthesis, including 6 components of the mur ligase pathway. Proteins associated with DNA synthesis were also affected by HT61 treatment as well as treatment with 16 mg/liter HT61 led to increased expression of proteins associated with DNA maintenance, including three protein with helicase activity (PcrA, GyrA, and ParE).; Reference: Antimicrob Agents Chemother. 2020 Apr 21;64(5):e02073-19. https://pubmed.ncbi.nlm.nih.gov/32122902/
• In Vivo Activity: In an attempt to develop HT61 as a topical agent to clear MSSA and MRSA, it was investigated if HT61 killed MSSA and MRSA on mouse skin. Log phase or stationary phase MSSA or MRSA were applied onto the intact skin of live mice at 107 CFU per 2 cm2 followed by immediate treatment with 45 µl of HY50A (gel containing 1% HT61) or 45 µl of Bactroban ointment (GlaxoSmithKline containing 2% mupirocin) or 45 µl of placebo. After two hours of treatment, HT61 removed 100% stationary phase MSSA and 93% stationary phase MRSA on the mouse skin. HT61 killed 55% of the bacteria on the skin for log phase MSSA.; Reference: PLoS One. 2010 Jul 27;5(7):e11818. https://pubmed.ncbi.nlm.nih.gov/20676403/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).