341329 Fatostatin - CAS 298197-04-3 - Calbiochem

341329
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₁₈H₁₈N₂S • HBr298197-04-3

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341329-25MGCN
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      25 mg
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      Description
      OverviewA cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 (Sterol Regulatory Element Binding Proteins 1/2) precursors to the active nuclear forms (>95% inhibition at 20 µM in CHO-K1 cells) by blocking SREBPs-SCAP (SREBP Cleavage-Activating Protein) ER to Golgi translocation with little effect against the transcription activity of the mature SREBPs. Binding studies employing recombinant SCAP truncation constructs reveal that Fatostatin targets SCAP between aa 448 to 767 in a reversible manner and is of no effect against SREBP-SCAP interaction. Fatostatin effectively suppresses SREBPs-dependent cellular functions in vitro, such as insulin-induced 3T3-L1 adipogenesis (complete inhibition at ≤20 µg/ml) and IGF1-dependent DU-145 proliferation (IC50 = 100 nM), and exhibits in vivo efficacy in lowering blood glucose level (by 70%) and body weight (by 12%) of ob/ob mice over a 28-day treatment period (30 mg/kg daily i.p.) without affecting animal food intake or apparent adverse effects.
      Catalogue Number341329
      Brand Family Calbiochem®
      Synonyms125B11, 2-Propyl-4-(4-(p-tolyl)thiazol-2-yl)pyridine, HBr, SREBP Processing Inhibitor II
      References
      ReferencesKamisuki, S., et al. 2009. Chem. Biol. 16, 882.
      Choi, Y., et al. 2003. J. Biol. Chem. 278, 7320.
      Product Information
      CAS number298197-04-3
      FormPale yellow solid
      Hill FormulaC₁₈H₁₈N₂S • HBr
      Chemical formulaC₁₈H₁₈N₂S • HBr
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Fatostatin - CAS 298197-04-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      341329

      References

      Reference overview
      Kamisuki, S., et al. 2009. Chem. Biol. 16, 882.
      Choi, Y., et al. 2003. J. Biol. Chem. 278, 7320.
      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.

      Revision08-April-2011 RFH
      Synonyms125B11, 2-Propyl-4-(4-(p-tolyl)thiazol-2-yl)pyridine, HBr, SREBP Processing Inhibitor II
      DescriptionA cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 (Sterol Regulatory Element Binding Proteins 1/2) precursors to the active nuclear forms (>95% inhibition at 20 µM in CHO-K1 cells) by blocking SREBPs-SCAP (SREBP Cleavage-Activating Protein) ER to Golgi translocation with little effect against the transcription activity of the mature SREBPs. Binding studies employing recombinant SCAP truncation constructs reveal that Fatostatin targets SCAP between aa 448 to 767 in a reversible manner and is of no effect against SREBP-SCAP interaction. Fatostatin effectively suppresses SREBPs-dependent cellular functions in vitro, such as insulin-induced 3T3-L1 adipogenesis (complete inhibition at ≤20 µg/ml) and IGF1-dependent DU-145 proliferation (IC50 = 100 nM), and exhibits in vivo efficacy in lowering blood glucose level (by 70%) and body weight (by 12%) of ob/ob mice over a 28-day treatment period (30 mg/kg daily i.p.) without affecting animal food intake or apparent adverse effects.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number298197-04-3
      Chemical formulaC₁₈H₁₈N₂S • HBr
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKamisuki, S., et al. 2009. Chem. Biol. 16, 882.
      Choi, Y., et al. 2003. J. Biol. Chem. 278, 7320.