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Home > Endocrinology/Hormones > Androgen Receptor > Galeterone

Galeterone

Catalog No. T6509    CAS 851983-85-2    Synonyms: TOK-001, VN/124-1, VN 124

Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

Pack Size Availability Price/USD Quantity
5 mg In Stock 60.00
10 mg In Stock 90.00
25 mg In Stock 162.00
50 mg In Stock 270.00
100 mg In Stock 450.00
1 mL * 10 mM (in DMSO) In Stock 60.00
Bulk Size: Please Quote for Discount Please Quote for Bulk Size
Biological Activity:

Product Description:

Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

Receptor:

Androgen Receptor; CYP17;

Chemical Information:
Molecular Weight 388.55
Formula C26H32N2O
CAS Number 851983-85-2
Solubility

DMSO: 19.4 mg/mL (50 mM)

Ethanol: 19.4 mg/mL (50 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )
Storage 3 years -20°C powder;
2 years -80°C in solvent;
Remark For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20 ℃ for several month.