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533683 C5aR Antagonist, PMX53 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₄₇H₆₅N₁₁O₇·TFA

Products

Catalog NumberPackaging Qty/Pack
5.33683.0001 Glass bottle 10 mg
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
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
Catalog Number GTIN
5.33683.0001 04055977286632

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 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.