product name Andarine
Description: Andarine, also known as GTx-007 and S-4, is an orally active, selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Andarine is an investigational drug that has the potential for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects.
References: J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40; Endocrinology. 2004 Dec;145(12):5420-8.
441.36
Formula
C19H18F3N3O6
CAS No.
401900-40-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 88 mg/mL (199.4 mM)
Water: <1 mg/mL
Ethanol: 88 mg/mL (199.4 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL
Synonyms
GTx-007
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394701
| In Vitro |
In vitro activity: Andarine stimulates AR-mediated transcription to 93% of that observed for 1 nM DHT at a concentration of 10 nM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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. Besides, Andarine shows no dose-dependent effect on castration-induced change in FSH, and partially suppresses LH production at dose rates of 0.5 mg/day or higher. In dogs administrated by intravenous doses of Andarine (0.1, 1, 3, and 10 mg/kg), the total body clearance (CL) ranged from 7.4 mL/min/kg to 3.1 mL/min/kg, volume of distribution at steady state (Vss) is 1.39 L/kg and half-life of Andarine is 229 minutes, respectively. In addition, oral bioavailability is 38%, 62% and 91% for the 10 mg/kg, 1 mg/kg and 0.1 mg/kg doses, respectively. 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. |
| Animal model | Male Sprague-Dawley rats and castrated rat model. |
| Formulation & Dosage | Dissolved in minimal amounts of ethanol and then diluted to final concentrations with PEG 300; ≤1 mg/day; Administered via osmotic pump. |
| References | J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40; Endocrinology. 2004 Dec;145(12):5420-8. |
Related Posts
product name Andarine
Description: Andarine, also known as GTx-007 and S-4, is an orally active, selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Andarine is an investigational drug that has the potential for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects.
References: J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40; Endocrinology. 2004 Dec;145(12):5420-8.
441.36
Formula
C19H18F3N3O6
CAS No.
401900-40-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 88 mg/mL (199.4 mM)
Water: <1 mg/mL
Ethanol: 88 mg/mL (199.4 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL
Synonyms
GTx-007
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394701
| In Vitro |
In vitro activity: Andarine stimulates AR-mediated transcription to 93% of that observed for 1 nM DHT at a concentration of 10 nM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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. Besides, Andarine shows no dose-dependent effect on castration-induced change in FSH, and partially suppresses LH production at dose rates of 0.5 mg/day or higher. In dogs administrated by intravenous doses of Andarine (0.1, 1, 3, and 10 mg/kg), the total body clearance (CL) ranged from 7.4 mL/min/kg to 3.1 mL/min/kg, volume of distribution at steady state (Vss) is 1.39 L/kg and half-life of Andarine is 229 minutes, respectively. In addition, oral bioavailability is 38%, 62% and 91% for the 10 mg/kg, 1 mg/kg and 0.1 mg/kg doses, respectively. 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. |
| Animal model | Male Sprague-Dawley rats and castrated rat model. |
| Formulation & Dosage | Dissolved in minimal amounts of ethanol and then diluted to final concentrations with PEG 300; ≤1 mg/day; Administered via osmotic pump. |
| References | J Pharmacol Exp Ther. 2003 Mar;304(3):1334-40; Endocrinology. 2004 Dec;145(12):5420-8. |