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  3. PMX 53 monoacetate

PMX 53 monoacetate (3D53 monoacetate) is a potent orally active CD88 (C5aR) antagonist that inhibits C5a-induced neutrophil myeloperoxide release and chemotactic activity. PMX 53 monoacetate has an IC50 value of 20 nM against C5a-induced neutrophil myeloperoxide release. >The value is 22 nM, and the IC50 value of the chemotactic activity is 75 nM. PMX 53 monoacetate is also an agonist of MrgX2.

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CAS No. : 852629-88-0

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Based on 8 publication(s) in Google Scholar

Other Forms of PMX 53 monoacetate:

Top Publications Citing Use of Products

    PMX 53 monoacetate purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523.  [Abstract]

    Chemotaxis of THP1 cells toward medium without FBS (control), medium without FBS + 0.1 μg/mL of C5a (C5a), and THP1 cells pre-treated 30 min with 0.9 μg/mL PMX53 toward medium without FBS + 0.1 μg/mL C5a (PMX53 + C5a) was evaluated. After 2 h of migration, RFU (Ex/Em = 485/520 nm) was measured.

    PMX 53 monoacetate purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523.  [Abstract]

    Western blotting of phosphoS6, phosphoHSP27, phosphoERK, and the loading control β-actin of THP1 cells untreated or treated with PMX53 (0.9 μg/mL) and/or C5a for 30 min. The experiment was performed three times with similar results.

    PMX 53 monoacetate purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523.  [Abstract]

    Chemotaxis of primary monocytes isolated from WT and C5aR1-/- mice toward medium without FBS, medium without FBS + 0.1 μg/mL of C5a (C5a). Migration of WT monocytes pre-treated for 30 min with 0.9 μg/mL PMX53 toward medium without FBS + 0.1 μg/mL C5a was also evaluated n = 4–6.

    PMX 53 monoacetate purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523.  [Abstract]

    Schematic representation of the pharmacological inhibition of C5aR1 in the DoxoR-induced senescence model. At day 0, 15-week-old mice received either vehicle or DoxoR (10 mg/kg, i.p.). From day 1 to day 30, mice received PMX53 (1 mg/kg, daily subcutaneous) or vehicle 2.

    PMX 53 monoacetate purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Aug 2;31(8):2507-2523.  [Abstract]

    Schematic representation of the pharmacological inhibition of C5aR1 in the DoxoR-induced senescence model. At day 0, 15-week-old mice received either vehicle or DoxoR (10 mg/kg, i.p.). From day 1 to day 30, mice received PMX53 (1 mg/kg, daily subcutaneous) or vehicle 2. Quantitative parameters and 3D representation of the cortical bone of tibiae measured by μ-CT.

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    Description

    PMX 53 monoacetate (3D53 monoacetate) is a potent orally active CD88 (C5aR) antagonist that inhibits C5a-induced neutrophil myeloperoxide release and chemotactic activity. PMX 53 monoacetate has an IC50 value of 20 nM against C5a-induced neutrophil myeloperoxide release. >The value is 22 nM, and the IC50 value of the chemotactic activity is 75 nM. PMX 53 monoacetate is also an agonist of MrgX2[1].

    Molecular Weight

    956.14

    Formula

    C49H69N11O9

    CAS No.
    SMILES

    CC(O)=O.O=C([C@H](NC([C@@]1([H])N(CCC1)C([C@H](CCCNC([C@@H](NC2=O)CCCNC(N)=N)=O)NC([C@@H](NC(C)=O)CC3=CC=CC=C3)=O)=O)=O)CC4CCCCC4)N[C@H]2CC5=CNC6=CC=CC=C56

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    Product Name:
    PMX 53 monoacetate
    Cat. No.:
    HY-106178D
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