MedKoo Cat#: 129095 | Name: E6742

Description:

WARNING: This product is for research use only, not for human or veterinary use.

E6742 is a TLR 7/8 antagonist.

Chemical Structure

E6742
E6742
CAS#N/A

Theoretical Analysis

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

Price and Availability

Related CAS #
No Data
Synonym
E6742; E-6742; E 6742
IUPAC/Chemical Name
(2R,6R)-4-(8-cyanoquinolin-5-yl)-N-((3S,4R)-4-fluoropyrrolidin-3-yl)-6-methylmorpholine-2-carboxamide
InChi Key
BLEGXEJTJXNGSC-GMLZMKKNSA-N
InChi Code
InChI=1S/C20H22FN5O2/c1-12-10-26(11-18(28-12)20(27)25-16-9-23-8-15(16)21)17-5-4-13(7-22)19-14(17)3-2-6-24-19/h2-6,12,15-16,18,23H,8-11H2,1H3,(H,25,27)/t12-,15-,16+,18-/m1/s1
SMILES Code
C[C@H](C1)O[C@@H](C(N[C@@H]2[C@H](F)CNC2)=O)CN1C3=CC=C(C#N)C4=NC=CC=C43
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
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.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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.