PMX-53 (Synonyms: 3D53)

Name: PMX-53
Brand: MedChemExpress
SKU: HY-106178
Rating: 5.0 (8 reviews)

Cat. No.: HY-106178 Purity: 99.95%: Data Sheet
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PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC₅₀ of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

CAS No. : 219639-75-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of PMX-53:

PMX 53 monoacetate Get quote

8 Publications Citing Use of MCE PMX-53

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: PMX-53 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 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 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 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 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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Biological Activity
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References
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Description

IC₅₀ & Target

IC50: 20 nM (Complement C5a receptor)^[4]
MrgX2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.104 μM Compound: 1, PMX53	Inhibition of C5a binding to human C5aR expressed in HEK293 cells Inhibition of C5a binding to human C5aR expressed in HEK293 cells	[PMID: 16876401]
J774.A1	IC₅₀	7.1 μM Compound: 1, PMX53	Inhibition of C5a-induced chemotaxis of mouse J774A.1 cells Inhibition of C5a-induced chemotaxis of mouse J774A.1 cells	[PMID: 16876401]

In Vitro

PMX-53 is a potent CD88 antagonist and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC₅₀ values of 22 nM and 75 nM, respectively^[1].
PMX-53 (10 nM) inhibits C5a-induced Ca²⁺ mobilization in HMC-1 cells, but at higher concentrations( ≥30 nM) it causes degranulation in LAD2 mast cells, CD34⁺ cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2. Replacement of Trp with Ala and Arg with dArg abolishes the ability of PMX-53 to inhibit C5a-induced Ca²⁺ mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PMX-53 (0.3-3 mg/kg; subcutaneous injection; once; male Wistar rats) treatment inhibits the hypernociception induced by zymosan-activated serum and C5a but not by the direct-acting hypernociceptive mediators, prostaglandin E2 and dopamine^[2].
Local pretreatment of rats with PMX-53 (60-180 μg per paw) inhibits zymosan-, carrageenan-, lipopolysaccharide (LPS)- and antigen-induced hypernociception^[2].
Pharmacokinetic analyses have shown that PMX-53 (3D53) appears in the plasma within 5 min of oral administration (3 mg/kg) to rats, with peak blood levels of approximately 0.3 μM being reached within 20 min The plasma elimination half-life was approximately 70 min in this case^[3].
The non-acetylated version of PMX-53 (3D53) binds to isolated mouse neutrophils with a K_d value of 30 nM (mouse C5a binds with a K_d value of 0.3 nM) and inhibits mouse C5a-induced chemotaxis with an IC₅₀ value of 0.5 nM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male Wistar rats (weighing 180-200 g) injected with zymosan^[2]
Dosage:	0.3 mg/kg, 1 mg/kg or 3 mg/kg
Administration:	Subcutaneous injection; once
Result:	Inhibited the hypernociception induced by zymosan-activated serum and C5a.

Molecular Weight

896.09

Formula

C₄₇H₆₅N₁₁O₇

CAS No.

219639-75-5

Appearance

Solid

Color

White to off-white

Sequence

Ac-Phe-{Orn}-Pro-{dCha}-Trp-Arg (Lactam bridge: Orn2-Arg6)

Sequence Shortening

Ac-F-{Orn}-P-{dCha}-WR (Lactam bridge: Orn2-Arg6)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (111.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 50 mg/mL (55.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1160 mL	5.5798 mL	11.1596 mL
5 mM	0.2232 mL	1.1160 mL	2.2319 mL
10 mM	0.1116 mL	0.5580 mL	1.1160 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (288 KB) SDS (252 KB)

COA (260 KB) HNMR (351 KB) RP-HPLC (247 KB) LCMS (91 KB) Elemental Analysis Report (119 KB)

Handling Instructions (2659 KB)

References

[1]. Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13. [Content Brief]

[2]. Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153(5):1043-53. [Content Brief]

[3]. Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73. [Content Brief]

[4]. Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42(11):1965-74. [Content Brief]

[5]. Manthey HD, et al. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J. 2011 Jul;25(7):2447-55. [Content Brief]

[6]. Vadrevu SK, et al. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 2014 Jul 1;74(13):3454-65. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.1160 mL	5.5798 mL	11.1596 mL	27.8990 mL
	5 mM	0.2232 mL	1.1160 mL	2.2319 mL	5.5798 mL
	10 mM	0.1116 mL	0.5580 mL	1.1160 mL	2.7899 mL
	15 mM	0.0744 mL	0.3720 mL	0.7440 mL	1.8599 mL
	20 mM	0.0558 mL	0.2790 mL	0.5580 mL	1.3949 mL
	25 mM	0.0446 mL	0.2232 mL	0.4464 mL	1.1160 mL
	30 mM	0.0372 mL	0.1860 mL	0.3720 mL	0.9300 mL
	40 mM	0.0279 mL	0.1395 mL	0.2790 mL	0.6975 mL
	50 mM	0.0223 mL	0.1116 mL	0.2232 mL	0.5580 mL
DMSO	60 mM	0.0186 mL	0.0930 mL	0.1860 mL	0.4650 mL
	80 mM	0.0139 mL	0.0697 mL	0.1395 mL	0.3487 mL
	100 mM	0.0112 mL	0.0558 mL	0.1116 mL	0.2790 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

PMX-53 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PMX-53 (Synonyms: 3D53)

Customer Review

Other Forms of PMX-53:

PMX-53 Related Antibodies

8 Publications Citing Use of MCE PMX-53

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•Related Screening Libraries:

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Biological Activity

Purity & Documentation

References

Customer Review

PMX-53 Related Antibodies

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Complete Stock Solution Preparation Table

PMX-53 Related Classifications

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