Izonsteride

SKU: orb1700312

Description

Izonsteride (LY320236) is a potent dual inhibitor of 5α-reductase types I and II. It is applied in research for prostate cancer and genitourinary disorders, with utility in both in vitro enzymatic assays and in vivo models of disease progression.

Research Area

Metabolism Research

Key Properties

• CAS Number: 176975-26-1
• MW: 422.61
• Purity: 99.55% (May vary between batches)
• Formula: C₂₄H₂₆N₂OS₂
• SMILES: C[C@@]12C=3C(=CC(SC4=NC=5C(S4)=CC=CC5CC)=CC3)CC[C@]1(N(C)C(=O)CC2)[H]
• Target: Reductase
• Solubility: DMSO:6.88 mg/mL (16.28 mM)

Bioactivity

• In Vitro:
  Izonsteride is a benzoquinolinone (BQ) that inhibits 5alpha-R activity in human scalp skin (Ki(typeI)=28.7+/-1.87 nM) and prostatic homogenates (Ki(typeII)=10.6+/-4.5 nM). Lineweaver-Burk, Dixon, and non-linear analysis methods were used to evaluate the kinetics of 5alpha-R inhibition by Izonsteride. Non-linear modeling of experimental data evaluated V(max) in the presence or absence of Izonsteride. Experimental data modeled to the following equation 1v=+ fixing the In0c value equal to 1.0 or 0 are consistent with non-competitive or competitive inhibition, respectively. Izonsteride is a competitive inhibitor of type I 5alpha-R (In0c=0, Ki=3.39+/-0.38, RMSE = 1.300) and a non-competitive inhibitor of type II 5alpha-R (In0c=1, Ki=29. 7+/-3.4, RMSE = 0.0592). These data are in agreement with the linear transformation of the data using Lineweaver-Burk and Dixon analyses. These enzyme kinetic data support the contention that the BQ Izonsteride is a potent dual inhibitor with differing modes of activity against the two known human 5-alpha-reductase isozymes. Izonsteride represents a class of non-steroidal 5alpha-R inhibitors with potential therapeutic utility in treating a variety of androgen-dependent disorders.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-α reductase, LY 320236, LY320236, LY-320236, Izonsteride, UNII-A5E8C36F34

Compound Identifiers

PubChem CID

172988