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Chemical Structure| 219639-75-5 Chemical Structure| 219639-75-5

Structure of PMX-53
CAS No.: 219639-75-5

Chemical Structure| 219639-75-5

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PMX 53 is a potent C5a receptor antagonist.

Synonyms: 3D53

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Product Details of PMX-53

CAS No. :219639-75-5
Formula : C47H65N11O7
M.W : 896.09
SMILES Code : O=C([C@H](CCCNC(N)=N)NC([C@H](CC1=CNC2=CC=CC=C21)NC([C@@H](CC3CCCCC3)NC([C@]4([H])CCCN54)=O)=O)=O)NCCC[C@H](NC([C@@H](NC(C)=O)CC6=CC=CC=C6)=O)C5=O
Synonyms :
3D53
MDL No. :MFCD07363866

Safety of PMX-53

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Infantile spasms model Subcutaneous injection 0.6 mg/kg Once daily for 4 days To evaluate the therapeutic effect of PMX53 on infantile spasms, results showed PMX53 significantly reduced the number of spasms Sci Rep. 2018 Apr 10;8(1):5722
Rats Reverse passive Arthus reaction model Oral, intravenous or topical 1 – 10 mg/kg Single dose, 30 min prior (oral) or 10 min prior (intravenous or topical) Inhibited immune-complex mediated dermal vascular leakage and systemic cytokine production Br J Pharmacol. 2001 Dec;134(8):1778-86
Mice MC-38 colorectal cancer model Intravenous injection 1 mg/kg Every other day until the end of the experiment Evaluated the antitumor effect of PMX-53, demonstrating that PMX-53 suppressed CRC growth by modulating gut microbiota and TLR5/AKT2 pathway to promote M1 polarization. Cell Death Dis. 2024 Feb 8;15(2):120
Mice NASH model Intraperitoneal injection 1 mg/kg Every other day for 4 weeks To evaluate the effect of PMX-53 on liver inflammation and fibrosis in NASH mice J Gastroenterol. 2023 Sep;58(9):894-907
Mice Chronic graft-versus-host disease (cGVHD) model Intraperitoneal injection 1 mg/kg Every three days PMX53 treatment attenuated the pathology of cGVHD, improved the survival rate of mice, and increased the frequency of Treg and expression of TGF-β1 Sci Rep. 2017 Jun 15;7(1):3603
Mice K14-HPV16 transgenic mice Subcutaneous implantation 1.0 mg/kg/day Once daily for 28 days PMX-53 in combination with paclitaxel significantly slowed the growth of squamous cell carcinomas, increased infiltration and cytotoxic properties of CXCR3+ effector memory CD8+ T cells Cancer Cell. 2018 Oct 8;34(4):561-578. e6
Mice Bullous pemphigoid model Intraperitoneal injection 200 µg/mouse Daily for 12 days To evaluate the effect of PMX-53 in prophylactic and therapeutic settings, results showed reduced skin lesions in prophylactic but not therapeutic approach. Front Immunol. 2018 Mar 15;9:488
Mice Hind paw incision model Subcutaneous injection 30 mcg/paw 2 hours before surgery and daily 2 hours before behavioral testing PMX53 reduced incisional mechanical and heat nociceptive sensitization regardless of neutrophil depletion Anesthesiology. 2012 Sep;117(3):602-12
Mice Hind paw incisional model Intraplantar injection 30 μg/15 μl Injected 1 hour before incision and then 2 hours before each test session To evaluate the effect of PMX53 on incision-induced heat hyperalgesia and mechanical allodynia, results showed that PMX53 significantly attenuated heat hyperalgesia and mechanical allodynia induced by hind paw incision J Neuroinflammation. 2011 Jul 7;8:80
Rats and mice Mechanical hypernociception model Intraplantar injection (rats), subcutaneous injection (mice) 60–180 μg per paw (rats), 0.3–3 mg/kg (mice) Single administration, observed for 1–24 h PMX53 inhibited hypernociception induced by zymosan, carrageenan, LPS, and antigen, associated with C5a receptor blockade Br J Pharmacol. 2008 Mar;153(5):1043-53

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.12mL

0.22mL

0.11mL

5.58mL

1.12mL

0.56mL

11.16mL

2.23mL

1.12mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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