E6446

• Catalog Number: ACM1219925731
• Product Name: E6446
• CAS: 1219925-73-1
• Category: Inhibitors
• Description: E6446 is a TLR inhibitor. E6446 inhibits Toll-like receptor (TLR)7 and 9 signaling. E6446 works in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro. When administered to mice, this compound suppress responses to challenge doses of cytidine-phosphate-guanidine (CpG)-containing DNA, which stimulates TLR9.
• Synonyms: E6446; E 6446; E-6446
• IUPAC Name: 6-(3-Pyrrolidin-1-yl-propoxy)-2-[4-(3-pyrrolidin-1-yl-propoxy)-phenyl]-benzooxazole
• Molecular Weight: 449.60
• Molecular Formula: C27H35N3O3
• Canonical SMILES: C1(C2=CC=C(OCCCN3CCCC3)C=C2)=NC4=CC=C(OCCCN5CCCC5)C=C4O1
• InChI: InChI=1S/C27H35N3O3/c1-2-14-29(13-1)17-5-19-31-23-9-7-22(8-10-23)27-28-25-12-11-24(21-26(25)33-27)32-20-6-18-30-15-3-4-16-30/h7-12,21H,1-6,13-20H2
• InChI Key: YMYJXFUPMPMETB-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).
• Alternative CAS: 1345675-25-3 (HCl); 1219925-73-1 (free base)
• Biological Target: E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 72.13; H, 7.85; N, 9.35; O, 10.68
• Exact Mass: 449.2678
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: Measurement of ELAM-1-luciferase activity showed that E6446 specifically inhibited TLR9 activation with CpG ODN 2006, in the range of 0.01-0.03 μM. A 100-fold higher concentration (2-8 μM) of E6446 was required to inhibit TLR7/8 activated by the imidazoquinoline compound R848. Incubation of cells with even higher concentrations (30 μM) of E6446 was required to reduce 50% of TLR4 activation (Fig. 2A).; Reference: Proc Natl Acad Sci U S A. 2011 Mar 1; 108(9): 3689-3694. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3048158/
• In Vivo Activity: E6446 treatment significantly reduced LV chamber size and improved cardiac function in TAC-operated mice.; Reference: JACC Basic Transl Sci. 2019 Jun; 4(3): 348-363. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6610159/
• 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).