Andarine (GTX-007) is a selective nonsteroidal androgen receptor (AR) agonist with Ki of 4 nM. It is an investigational selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy, using the non-steroidal androgen antagonist bicalutamide as a lead compound. Andarine is less potent in both anabolic and androgenic effects than other SARMs. Andarine exhibits potent and efficacious anabolic activity and results in dose-dependent stimulation of growth in prostate, seminal vesicles, and levator ani muscle with the ED50 of 0.43 mg/day, 0.55 mg/day, and 0.14 mg/day, respectively. Andarine reduced prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects. Andarine demonstrates tissue-selective pharmacological activity and significantly decreased prostate weight to 79.4% at a concentration of 0.5 mg/day in intact rats. Andarine (GTx-007) is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist effects at androgen receptors prevent the side effects associated with the anti-androgenic drugs traditionally used for treatment of BPH.
| Molecular Weight | 441.36 |
| Formula | C19H18F3N3O6 |
| CAS Number | 401900-40-1 |
| Solubility (25°C) | DMSO 80 mg/mL Ethanol 80 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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