| Identification | Back Directory | [Name]
3H-1-Benzazepine-4-carboxylic acid, 2-aMino-8-(3-cyanophenyl)-, ethyl ester | [CAS]
1268163-15-0 | [Synonyms]
TL8-506
YHRYTTWRVKXODS-UHFFFAOYSA-N
3H-1-Benzazepine-4-carboxylic acid, 2-aMino-8-(3-cyanophenyl)-, ethyl ester | [Molecular Formula]
C20H17N3O2 | [MDL Number]
MFCD28359121 | [MOL File]
1268163-15-0.mol | [Molecular Weight]
331.37 |
| Chemical Properties | Back Directory | [Boiling point ]
566.1±60.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
-10 to -25°C | [solubility ]
DMSO: 2mg/mL, clear (Warmed) | [form ]
Solid | [pka]
-0.87±0.40(Predicted) | [color ]
Light yellow to light brown | [InChI]
InChI=1S/C20H17N3O2/c1-2-25-20(24)17-9-16-7-6-15(10-18(16)23-19(22)11-17)14-5-3-4-13(8-14)12-21/h3-10H,2,11H2,1H3,(H2,22,23) | [InChIKey]
YHRYTTWRVKXODS-UHFFFAOYSA-N | [SMILES]
N1C2=CC(C3=CC=CC(C#N)=C3)=CC=C2C=C(C(OCC)=O)CC=1N |
| Hazard Information | Back Directory | [Uses]
TL8-506 is a specific TLR8 agonist with an EC50 of 30?nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy[1][2]. | [Biological Activity]
TL8-506 is a motolimod (VTX-2337) analog and a benzoazepine class toll-like receptor 8 (TLR8)-selective agonist. TL8-506 is commonly employed in the concentration range from 0.1 μg/mL to 1 μg/mL for stimulating cell surface TLR8 in cultures and is reported to be a stronger TLR8 ligand than the imidazoquinoline (IMDQ) derivatives (IQDs) resiquimod (R848) and CL075 (3M002). | [in vivo]
TL8-506 (intramuscular injection; twice; four weeks apart)
can enhance the resistance to mycobacterium tuberculosisinfection in TLR8 transgenic mice(TL8-506 and ESAT-6, aluminum hydroxide vaccine)[2]. | Animal Model: | Mtb H37Rv treated female TLR8 transgenic mice aged 6 weeks old[2] | | Dosage: | Twice, four weeks apart | | Administration: | Intramuscular injection (i.m.); TL8-506 was in form of ESAT6-Alum-TL8-506. | | Result: | Provided better protection against Mtb challenge compared to ESAT6-Alum. The CFU in the lungs of mice treated with ESAT6-Alum-TL8-506 was significantly lower than that in the ESAT6-Alum group.
Significantly lowered bacterial load in the lungs and livers of mice.
Significantly ameliorated the tuberculous pneumonia and alveolitis and reduced the numbers and the area of granulomas.
Significantly increased the proportion of central memory CD8+ T cells. |
| [IC 50]
TLR8: 30 nM (EC50) | [References]
[1] Jun Tang, et al. Toll-Like Receptor 8 Agonist Strengthens the Protective Efficacy of ESAT-6 Immunization to Mycobacterium tuberculosis Infection. Front Immunol. 2018 Jan 24;8:1972. DOI:10.3389/fimmu.2017.01972
[2] He M, S, et al. Combinations of Toll-like receptor 8 agonist TL8-506 activate human tumor-derived dendritic cells. J Immunother Cancer. 2022 Jun;10(6):e004268. DOI:10.1136/jitc-2021-004268 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|