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

385585
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₂BrNO₃S₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      385585-10MG
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          Glass bottle 10 mg
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          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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.