554726 | REV-ERB Agonist II, SR9009 - Calbiochem

554726
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₀H₂₄ClN₃O₄S

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      554726-25MG
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          25 mg
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          Description
          Overview A pyrrolidinecarbamate compound that acts as a specific REV-ERB-α/β agonist. Exhibits a direct and reversible binding (Kd = 800 nM REV-ERB-α) and shows excellent selectivity over a panel of 46 other nuclear receptors. Potently increases REV-ERB-dependent repressor activity (IC50 = 670 and 800 nM in Gal4-REV-ERB-α and β transfected HEK 293 cells) and reduces BMAL1 mRNA in HepG2 cells (IC50 = 710 nM). Shown to cross the blood-brain barrier and exhibit desirable pharmacokinetic properties. A 7-day administration of SR9009 (100 mg/kg, i.p., b.i.d.) causes a significant weight and fat loss in C57BL6 mice with concomitant reduction in plasma glucose and free fatty acid levels, and alters circadian pattern.
          Catalogue Number 554726
          Brand Family Calbiochem®
          Synonyms Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate
          References
          References Solt, L.A., et al. 2012. Nature 485, 62.
          Product Information
          Form Dark brown liquid
          Hill Formula C₂₀H₂₄ClN₃O₄S
          Molar Mass 437.9
          Reversible Y
          Structure formula Image
          Applications
          Biological Information
          Primary Target REV-ERB-α/&beta
          Purity ≥96% by HPLC
          Physicochemical Information
          Cell permeable Y
          Solubility DMSO
          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 No
          Special Instructions Following 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

          MSDS

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          Certificates of Analysis

          TitleLot Number
          554726

          References

          Reference overview
          Solt, L.A., et al. 2012. Nature 485, 62.
          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.

          Revision 16-November-2012 JSW
          Synonyms Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate
          Description A pyrrolidinecarbamate compound that acts as a specific REV-ERB-α/β agonist. Exhibits a direct and reversible binding (Kd = 800 nM REV-ERB-α) and shows excellent selectivity over a panel of 46 other nuclear receptors. Potently increases REV-ERB-dependent repressor activity (IC50 = 670 and 800 nM in Gal4-REV-ERB-α and β transfected HEK 293 cells) and reduces BMAL1 mRNA in HepG2 cells (IC50 = 710 nM). Shown to cross the blood-brain barrier and exhibit desirable pharmacokinetic properties. A 7-day administration of SR9009 (100 mg/kg, i.p., b.i.d.) causes a significant weight and fat loss in C57BL6 mice with concomitant reduction in plasma glucose and free fatty acid levels, and alters circadian pattern.
          Form Dark brown liquid
          Intert gas (Yes/No) Packaged under inert gas
          Molar mass 437.9
          Structure formula
          Purity ≥96% by HPLC
          Solubility DMSO (50 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          References Solt, L.A., et al. 2012. Nature 485, 62.