A non-steroidal inhibitor of the 17

Orteronel – 5 mg

Brand:
Cayman
CAS:
566939-85-3
Storage:
-20
UN-No:
Non-Hazardous - /

Orteronel is a non-steroidal inhibitor of the 17,20-lyase activity of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 48 and 19 nM for the rat and human enzyme, respectively), which is the CYP17A1 activity that converts progestogens into androgens.{39593} Orteronel is selective for the 17,20-lyase activity of CYP17A1 over its 11-hydroxylase activity and CYP3A4 (IC50s = >1,000 and >10,000 nM, respectively). It decreases adrenocorticotropic hormone-induced production of DHEA, androstenedione, cortisol, and aldosterone in monkey adrenal cells (IC50s = 110, 130, 310, and 4,400 nmol/L, respectively) and inhibits DHEA production in NCI-H295R human adrenocortical tumor cells.{39594} A single oral dose of orteronel (0.3-10 mg/kg) dose-dependently decreases DHEA, cortisol, and testosterone levels in the plasma of intact cynomolgus monkeys for at least 10 hours, and chronic dosing of 15 mg/kg twice daily suppresses levels for up to seven days of treatment. It also decreases DHEA and testosterone plasma levels in castrated monkeys, indicating an effect on extra-gonadal production of testosterone.  

 

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SKU: 24191 - 5 mg Category:

Description

A non-steroidal inhibitor of the 17,20-lyase activity of CYP17A1 (IC50s = 48 and 19 nM for the rat and human enzyme, respectively); selective for 17,20-lyase activity over 11-hydroxylase activity and CYP3A4 (IC50s = >1,000 and >10,000 nM, respectively); decreases ACTH-induced production of DHEA, androstenedione, cortisol, and aldosterone in monkey adrenal cells (IC50s = 110, 130, 310, and 4,400 nmol/L, respectively); inhibits DHEA production in NCI-H295R human adrenocortical tumor cells; decreases DHEA, cortisol, and testosterone levels in the plasma of intact cynomolgus monkeys for at least 10 hours following a single oral dose (0.3-10 mg/kg) and continuously during chronic dosing (15 mg/kg twice daily)

Formal name: 6-[(7S)-6,7-dihydro-7-hydroxy-5H-pyrrolo[1,2-c]imidazol-7-yl]-N-methyl-2-naphthalenecarboxamide

Synonyms:  TAK-700

Molecular weight: 307.3

CAS: 566939-85-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids||Research Area|Toxicology|Drug Metabolism|Cytochrome P450

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