Conditionnement : 100mg
Téléphone : +1 850 650 7790
Synonyms:
| Description | GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1]. |
| In vitro | GnRH-R antagonist 1 demonstrates a cell permeability that is 140 times greater than that of Relugolix, while also showing favorable stability in both human and mouse microsomes [1]. |
| In vivo | GnRH-R antagonist 1 administered orally at a dosage of 30 mg/kg once daily for seven days exhibits a good safety profile [1]. At a single oral dose of 12 mg/kg, it demonstrates favorable pharmacokinetics and high oral bioavailability, evident from a 44.7% F% value [1]. Furthermore, this dosage effectively suppresses circulating testosterone levels in rats for over 24 hours [1]. |
| Molecular Weight | 721.65 |
| Formula | C31H28F5N7O6S |
| Cas No. | 2826273-90-7 |
| Smiles | CN(CCOC(F)(F)F)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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