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GSK-2881078

Cat. No. M7561
GSK-2881078 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 250  USD250 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

GSK 2881078 is an androgen receptor regulator for the study of mental impotency.

Chemical Information
Molecular Weight 330.33
Formula C14H13F3N2O2S
CAS Number 1539314-06-1
Solubility (25°C) 33 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Charlotte Cutler, et al. Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes

[2] Katarzyna Kowalczyk, et al. In vitro metabolic studies of novel selective androgen receptor modulators and their use for doping control analysis

[3] Oliver Zierau, et al. Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay

[4] David Neil, et al. GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women

[5] Mario Thevis, et al. Mass spectrometric studies on selective androgen receptor modulators (SARMs) using electron ionization and electrospray ionization/collision-induced dissociation

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Keywords: GSK-2881078 supplier, Androgen Receptor, inhibitors, activators


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