AdipoRon is a novel, and orally bioavailable adiponectin receptor agonist with KD of 1.8 and 3.1 μM for AdipoR1 and AdipoR2, respectively.
 |
Source | Am J Physiol Endocrinol Metab (2015). Figure 2. AdipoRon |
| Method | Myocardial ischemia/reperfusion | |
| Cell Lines | APN knockout (APN-/-) mice | |
| Concentrations | 50 mg/kg | |
| Incubation Time | 24 h | |
| Results | Treatment with AdipoRon significantly improved cardiac functional recovery, as evidenced by increased LV ejection fraction |
 |
Source | Am J Physiol Endocrinol Metab (2015). Figure 1. AdipoRon |
| Method | Myocardial ischemia/reperfusion | |
| Cell Lines | APN knockout (APN-/-) mice | |
| Concentrations | 50 mg/kg | |
| Incubation Time | 24 h | |
| Results | Treatment with AdipoRon significantly improved cardiac functional recovery, as evidenced by improved maximal positive and negative dP/dt |
| Cell Experiment | |
|---|---|
| Cell lines | DG granule cells |
| Preparation method | A baseline recording of DG granule cells from WT mouse brain slices was first made followed by bath application of 15 μM AdipoRon, an AdipoR agonist that binds to both AdipoR1 and AdipoR2 with comparable high affinities. In response to depolarizing current injections (300 ms), AdipoRon treatment decreased the excitability of DG granule neurons, causing reduced number of action potentials elicited by current injections (60–90 pA), increased rheobase current and a more negative resting membrane potential without changing other membrane properties including input resistance, action potential threshold, fAHP and action potential waveforms. |
| Concentrations | 15 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | DMSO |
| Dosages | 50 mg/kg |
| Administration | oral |
| Molecular Weight | 428.52 |
| Formula | C27H28N2O3 |
| CAS Number | 924416-43-3 |
| Solubility (25°C) | DMSO 66 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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