533683 C5aR Antagonist, PMX53 - Calbiochem

533683
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₄₇H₆₅N₁₁O₇·TFA

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33683.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          Glass bottle 10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          Description
          OverviewA cell-permeable, orally available, and metabolically stable macrocyclic hexapeptidomimetic compound that acts as a non-competitive antagonist of complement C5a receptor (C5aR; CD88; IC50 = 240 nM) and as a low-affinity agonist for MrgX2, a GPCR, in human mast cells Shown to specifically bind to C5aR1 and not to CaR2 and C3aR. Displays a broad range of anti-inflammatory effects, both in vitro and in vivo. Shown to inhibit C5a-induced neutrophil myeloperoxidase release (IC50 = 22 nM) and chemotaxis (IC50 = 75 nM). Preincubation with PMX-53 (~10 nM) blocks C5a-induced Ca2+ responses in HMC-1 and RBL-2H3 cells, but does not affect C3a responses. Suppresses the growth of 4T1 mammary carcinoma tumor xenograft in mice (1 mg/kg/every 2-3 days, s.c.). Reported to diminish C5a-mediated increase in pluripotency in human embryonic stem cells in the absence of FGF2.
          Catalogue Number533683
          Brand Family Calbiochem®
          SynonymsAc-(cyclo-2,6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53
          DescriptionC5aR Antagonist, PMX53
          References
          ReferencesLillegard, K., et al. 2014. JPET. 351,344.
          Vadrevu, S. K., et al. 2014. Cancer Res. 74, 3454.
          Liang, S., et al. 2011. J. Immun. 186, 869.
          Woodruff, T., et al. 2005. JPET. 314, 811.
          Product Information
          FormOff-white solid
          Hill FormulaC₄₇H₆₅N₁₁O₇·TFA
          Chemical formulaC₄₇H₆₅N₁₁O₇·TFA
          ReversibleY
          Applications
          Biological Information
          Primary TargetC5aR
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Peptide SequenceAc-Phe-[Orn-Pro-dCha-Trp-Arg]
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          C5aR Antagonist, PMX53 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Lillegard, K., et al. 2014. JPET. 351,344.
          Vadrevu, S. K., et al. 2014. Cancer Res. 74, 3454.
          Liang, S., et al. 2011. J. Immun. 186, 869.
          Woodruff, T., et al. 2005. JPET. 314, 811.
          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-June-2016 JSW
          SynonymsAc-(cyclo-2,6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53
          DescriptionA cell-permeable, orally available, and metabolically stable macrocyclic hexapeptidomimetic compound that acts as a non-competitive antagonist of complement C5a receptor (C5aR; CD88; IC50 = 240 nM) and as a low-affinity agonist for MrgX2, a GPCR, in human mast cells Shown to specifically bind to C5aR1 and not to CaR2 and C3aR. Displays a broad range of anti-inflammatory effects, both in vitro and in vivo. Shown to inhibit C5a-induced neutrophil myeloperoxidase release (IC50 = 22 nM) and chemotaxis (IC50 = 75 nM). Preincubation with PMX-53 (~10 nM) blocks C5a-induced Ca2+ responses in HMC-1 and RBL-2H3 cells, but does not affect C3a responses. Suppresses the growth of 4T1 mammary carcinoma tumor xenograft in mice (1 mg/kg/every 2-3 days, s.c.). Reported to diminish C5a-mediated increase in pluripotency in human embryonic stem cells in the absence of FGF2.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₄₇H₆₅N₁₁O₇·TFA
          Peptide SequenceAc-Phe-[Orn-Pro-dCha-Trp-Arg]
          Purity≥98% 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesLillegard, K., et al. 2014. JPET. 351,344.
          Vadrevu, S. K., et al. 2014. Cancer Res. 74, 3454.
          Liang, S., et al. 2011. J. Immun. 186, 869.
          Woodruff, T., et al. 2005. JPET. 314, 811.