O-304 is a first-in-class, orally bioavailable pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. The drug O-304 has a lot of promise for treating type 2 diabetes (T2D) and its cardiovascular complications. References: Periodic Reporting for period 1-AMPK-DIAB ("A small molecule AMP activated protein kinase (AMPK) activator," denoted as "O304," as a novel, innovative drug for the treatment of type 2 diabetes).
Physicochemical Properties
| Molecular Formula | C16H11CL2N3O2S |
| Molecular Weight | 380.248440027237 |
| Exact Mass | 378.994 |
| Elemental Analysis | C, 50.54; H, 2.92; Cl, 18.65; N, 11.05; O, 8.42; S, 8.43 |
| CAS # | 1261289-04-6 |
| Related CAS # | 1261289-04-6 |
| PubChem CID | 50923806 |
| Appearance | White to off-white solid powder |
| LogP | 4.1 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 3 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 24 |
| Complexity | 516 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | WEDWLYRQKUTOAX-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C16H11Cl2N3O2S/c17-12-5-1-10(2-6-12)9-21-16(23)20-15(24-21)19-14(22)11-3-7-13(18)8-4-11/h1-8H,9H2,(H,19,20,22,23) |
| Chemical Name | 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide |
| Synonyms | O-304; O304; O 304 |
| 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
| Targets | AMPK |
| ln Vivo | O-304 boosts diet-induced intermittent beta cell rest, decreases beta cell prophase, and slightly increases muscle. O-304 decreased both the Hypoglycemic Model Assessment of Insulin Resistance (HOMA-IR) and fasting blood glucose levels in individuals with type 2 diabetes (T2D) included in a Phase IIa proof-of-concept clinical study using metformin [2]. |
| References |
[1]. Periodic Reporting for period 1-AMPK-DIAB (A small molecule AMP activated protein kinase (AMPK) activator, denoted O304, as a novelinnovative drug for the treatment of type 2 diabetes). |
Solubility Data
| Solubility (In Vitro) | DMSO: 20~30 mg/mL (52.6~78.9 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 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 is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6298 mL | 13.1492 mL | 26.2985 mL | |
| 5 mM | 0.5260 mL | 2.6298 mL | 5.2597 mL | |
| 10 mM | 0.2630 mL | 1.3149 mL | 2.6298 mL |