PeptideDB

TUG-2208

TUG-2208

CAS No.:

TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity, good solubility, in vitro permeability,
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TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity, good solubility, in vitro permeability, and microsomal stability.

Physicochemical Properties


Molecular Formula C16H12N2O3
Molecular Weight 280.28
Appearance Solid powder
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro TUG-2208 (0.1; 1 mM; 4; 96 h) showed excellent stability in rat liver microsomes[1]. TUG-2208 (10 μM) showed >1000-fold selectivity for GPR84 over other free fatty acid receptors (FFA1, FFA2, FFA3, FFA4)[1].
References

[1]. Structure-Activity Relationship Studies and Optimization of 4-Hydroxypyridones as GPR84 Agonists. J Med Chem. 2024 Feb 21.


Solubility Data


Solubility (In Vitro) DMSO : 100 mg/mL (356.79 mM; with sonication)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (8.92 mM)(Saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5679 mL 17.8393 mL 35.6786 mL
5 mM 0.7136 mL 3.5679 mL 7.1357 mL
10 mM 0.3568 mL 1.7839 mL 3.5679 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.