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533683 C5aR Antagonist, PMX53 - CAS 219639-75-5 - Calbiochem

A cell-permeable, orally available, non-competitive antagonist of C5a receptor (CD88; IC₅₀ = 240 nM) and as a low-affinity agonist for MrgX2.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Ac-(cyclo-2,6)-F-[OPdChaWR], C5aR Inhibitor, PMX53, C5a Receptor Inhibitor, PMX53, CD88 Inhibitor, PMX53, MrgX2 Agonist, PMX53

Primary Target: C5aR
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533683
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
219639-75-5C₄₇H₆₅N₁₁O₇·TFA

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      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
      CAS number219639-75-5
      FormOff-white solid
      Hill FormulaC₄₇H₆₅N₁₁O₇·TFA
      Chemical formulaC₄₇H₆₅N₁₁O₇·TFA
      ReversibleY
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5336830001 04055977286632

      Documentation

      C5aR Antagonist, PMX53 - CAS 219639-75-5 - 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
      CAS number219639-75-5
      Chemical formulaC₄₇H₆₅N₁₁O₇·TFA
      Peptide SequenceAc-Phe-[Orn-Pro-dCha-Trp-Arg]
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.