E6742 is a TLR 7/8 antagonist.
MedKoo Cat#: 129095
Name: E6742
CAS#: N/A
Chemical Formula: C20H22FN5O2
Exact Mass: 383.1758
Molecular Weight: 383.43
Elemental Analysis: C, 62.65; H, 5.78; F, 4.95; N, 18.27; O, 8.35
The following data is based on the product molecular weight 383.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Tanaka Y, Kumanogoh A, Atsumi T, Ishii T, Tago F, Aoki M, Yamamuro S, Akira
S. Safety, pharmacokinetics, biomarker response and efficacy of E6742: a dual
antagonist of Toll-like receptors 7 and 8, in a first in patient, randomised,
double-blind, phase I/II study in systemic lupus erythematosus. RMD Open. 2024
Sep 17;10(3):e004701. doi: 10.1136/rmdopen-2024-004701. PMID: 39289029; PMCID:
PMC11409405.
2: Yamakawa N, Tago F, Nakai K, Kitahara Y, Ikari S, Hojo S, Hall N, Aluri J,
Hussein Z, Gevorkyan H, Maruyama T, Ishizaka S, Yagi T. First-in-Human Study of
the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of E6742, a
Dual Antagonist of Toll-like Receptors 7 and 8, in Healthy Volunteers. Clin
Pharmacol Drug Dev. 2023 Apr;12(4):363-375. doi: 10.1002/cpdd.1176. Epub 2022
Oct 11. PMID: 36219471.
3: Ishizaka ST, Hawkins L, Chen Q, Tago F, Yagi T, Sakaniwa K, Zhang Z, Shimizu
T, Shirato M. A novel Toll-like receptor 7/8-specific antagonist E6742
ameliorates clinically relevant disease parameters in murine models of lupus.
Eur J Pharmacol. 2023 Oct 15;957:175962. doi: 10.1016/j.ejphar.2023.175962. Epub
2023 Aug 5. PMID: 37544422.
4: Tanaka Y, Tago F, Yamakawa N, Aoki M, Yagi T, Akira S. A new therapeutic
target for systemic lupus erythematosus: the current landscape for drug
development of a toll-like receptor 7/8 antagonist through academia-industry-
government collaboration. Immunol Med. 2024 Mar;47(1):24-29. doi:
10.1080/25785826.2023.2264023. Epub 2023 Sep 29. PMID: 37772762.