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385585 17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor - Calbiochem

385585
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₇H₁₂BrNO₃S₂

Products

Catalogue NumberPackaging Qty/Pack
385585-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of testosterone by directly inhibiting 17β-HSD3- (17β-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of Δ4-dione C17 ketone in a Δ4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50 = 0.6, 6.0, and 40 nM, respectively, against momoset, human, and mouse 17β-HSD3 activity in testes homogenate), and selective manner, displaying no activity against 17β-HSD1 and 17β-HSD2 activity. Poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only.
Catalogue Number385585
Brand Family Calbiochem®
Synonyms17β-HSD3 Inhibitor, 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxothiazolidin-4-one
References
ReferencesHarada, K., et al. 2012. Bioorg. Med. Chem. Lett. 22, 504.
Product Information
FormYellow solid
Hill FormulaC₁₇H₁₂BrNO₃S₂
Chemical formulaC₁₇H₁₂BrNO₃S₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

17β-Hydroxysteroid Dehydrogenase Type-3 Inhibitor - Calbiochem Certificates of Analysis

TitleLot Number
385585

References

Reference overview
Harada, K., et al. 2012. Bioorg. Med. Chem. Lett. 22, 504.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision24-September-2012 JSW
Synonyms17β-HSD3 Inhibitor, 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxothiazolidin-4-one
DescriptionA cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of the potent androgen testosterone by directly inhibiting 17β-HSD3- (17β-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of Δ4-dione C17 ketone in a Δ4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50 = 0.6, 6.0, and 40 nM, respectively, against momoset, human, and mouse 17β-HSD3 activity in testes homogenate; IC50 = 14 nM using 17β HSD3-transfected HeLa cells), and selective manner, displaying no activity against 17β-HSD1 and 17β-HSD2 activity in HeLa transfectants or AR- (andogen receptor), ERα- (estrogen receptor α), and GR- (glucocorticoid receptor) dependent transcription activities. Low aqueous solubility, lack of oral availability, and other poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₇H₁₂BrNO₃S₂
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml; pinkish solution)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesHarada, K., et al. 2012. Bioorg. Med. Chem. Lett. 22, 504.