In vitro, low doses of E6446 specifically inhibited the activation of human and mouse TLR9. E6446 suppress TLR9-DNA interaction in vitro, with an IC50 in the 1 to 10 µM range. E6446 reduces 50% of TLR4 activation at 30 μM, and shows IC50s of 0.01 μM and 0.23 μM in HEK-TLR9 cells stimulated with oligo 2006 and in human PBMCs stimulated with oligo 2216, respectively.
In vivo, therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection. E6446 (20, 60 mg/kg, p.o.) dose-dependently inhibits TLR9 signaling in mice.
Molecular Weight | 522.51 |
Formula | C27H37Cl2N3O3 |
CAS Number | 1345675-25-3 |
Solubility (25°C) | DMSO: ≥ 5 mg/mL (Need ultrasonic and warming) |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related TLR Products |
---|
Kdo2-Lipid A ammonium
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxic activity equivalent to LPS.Kdo2-Lipid A ammonium is highly selective for TLR4 and stimulates the release of TNF and PGE2. |
PSMα3
PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. |
Pam2CSK4
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. |
MAPK-IN-1
MAPK-IN-1 is a MAPK signaling pathway inhibitor. |
Cobitolimod
Cobitolimod is a first-of-its-kind (first-in-class), synthetic oligodeoxynucleotide (ODN) containing unmethylated CpG motifs that activates TLR9 in specific cells, including intestinal T and B lymphocytes as well as antigen-presenting cells (APCs), and can be used in studies related to inflammatory bowel disease (IBD). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.