567734 S1P₁ Receptor Agonist III - Calbiochem

567734
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      567734-10MG
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          Glass bottle 10 mg
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          Description
          OverviewAn orally bioavailable polar head group lacking carbamoylnicotinamide compound that acts as a potent and reversible agonist of hS1P1 receptor (EC50 = 35 nM with 96% efficacy) with substantial to excellent selectivity over hS1P5 (EC50 = 4.3 µM with 58% efficacy) and hS1P2-4 (EC50 > 25 µM). Minimally affects the activities of hERG (IC50 > 10 µM) and cytochrome p450 isozymes (IC50 > 30 µM for 3A4 and 2D6), and exhibits desirable microsomal stability and aqueous solubility, Shown to efficiently reduce the circulating lymphocyte levels in rats (1 mg/kg, p.o.).
          Catalogue Number567734
          Brand Family Calbiochem®
          Synonyms4-Methoxy-N-(2-(trifluoromethyl)biphenyl-4-ylcarbamoyl)nicotinamide, Sphingosine-1-Phosphate₁ Receptor Agonist III
          References
          ReferencesPennington, L.D., et al. 2011. Bioorg. Med. Chem. Lett. 22, 527.
          Product Information
          FormWhite solid
          Hill FormulaC₂₁H₁₆F₃N₃O₃
          Chemical formulaC₂₁H₁₆F₃N₃O₃
          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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          S1P₁ Receptor Agonist III - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Pennington, L.D., et al. 2011. Bioorg. Med. Chem. Lett. 22, 527.
          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.

          Revision30-November-2012 JSW
          Synonyms4-Methoxy-N-(2-(trifluoromethyl)biphenyl-4-ylcarbamoyl)nicotinamide, Sphingosine-1-Phosphate₁ Receptor Agonist III
          DescriptionAn orally bioavailable polar head group lacking carbamoylnicotinamide compound that acts as a potent and reversible agonist of hS1P1 receptor (EC50 = 35 nM with 96% efficacy) with substantial to excellent selectivity over hS1P5 (EC50 = 4.3 µM with 58% efficacy) and hS1P2-4 (EC50 > 25 µM). Minimally affects the activities of hERG (IC50 > 10 µM) and cytochrome p450 isozymes (IC50 > 30 µM for 3A4 and 2D6), and exhibits desirable microsomal stability and aqueous solubility, Shown to efficiently reduce the circulating lymphocyte levels in rats (1 mg/kg, p.o.).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₁H₁₆F₃N₃O₃
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml)
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesPennington, L.D., et al. 2011. Bioorg. Med. Chem. Lett. 22, 527.