| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
PMX-53 (3D53), a synthetic peptide, is a novel potent and orally bioactive dual C5aR(CD88) antagonist and Mas-related gene 2 (MrgX2) agonist. PMX-53 inhibits C5a-induced hypernociception in rats, inhibits lung metastasis in a mouse breast cancer model and reduces atherosclerotic lesions in a mouse model of atherosclerosis.
| ln Vitro |
With IC50 values of 22 nM and 75 nM, respectively, PMX-53 is a strong CD88 antagonist that blocks C5a-induced neutrophil myeloperoxidase release and chemotaxis [1]. PMX-53 (10 nM) prevents HMC-1 cells from being excited by C5a, but at concentrations greater than 30 nM, it promotes the degranulation of CD34+ cell-derived mast cells, MrgX2-expressing RBL cells, and LAD2 mast cells. Replacing Trp with Ala and Arg and PMX-53 with dArg prevented MrgX2-expressing RBL-2H3 cells from degranulating and prevented C5a-induced Ca2+ mobilization in HMC-1 cells [1].
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| ln Vivo |
Zymosin E2, which is the direct acting mediator of hypernociceptors, is not inhibited by PMX-53 (0.3–3 mg/kg; subcutaneous injection; once; Wistar staining) treatment. On the other hand, hypernociception caused by lever, carrageenan, lipopolysaccharide (LPS), reinforcement, and dopamine is inhibited by PMX-53 (60–180 μg per paw). After the warehouse powder (3 mg/kg) was administered, pharmacokinetic study revealed that PMX-53 (3D53) started to accumulate in the bones in 5 minutes and reached its maximum blood concentration of about 0.3 μM in 20 minutes. Here, the recession phase is divided in half, lasting roughly 70 minutes[3]. With a Kd of 30 nM, a non-chained variant of PMX-53 (3D53) binds to isolated mouse neutrophils (mouse C5a binding Kd).
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| Animal Protocol |
Animal/Disease Models: Adult male Wistar rat (body weight 180-200 g ) injection of zymosan [2]
Doses: 0.3 mg/kg is 0.3 nM) and inhibits C5a-induced chemotaxis in mice, with an IC50 value of 0.5 nM [3]. , 1 mg/kg or 3 mg/kg. Doses: subcutaneous injection; primary Experimental Results:inhibits excessive nociception caused by zymosan-activated serum and C5a. |
| References |
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| Molecular Formula |
C47H65N11O7
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|---|---|
| Molecular Weight |
896.088510274887
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| Exact Mass |
895.506
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| CAS # |
219639-75-5
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| PubChem CID |
6918468
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.684
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| LogP |
0.81
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
65
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| Complexity |
1680
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| Defined Atom Stereocenter Count |
6
|
| SMILES |
CC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@H]2CCCNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H]3CCCN3C2=O)CC4CCCCC4)CC5=CNC6=CC=CC=C65)CCCN=C(N)N
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| InChi Key |
YOKBGCTZYPOSQM-HPSWDUTRSA-N
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| InChi Code |
InChI=1S/C47H65N11O7/c1-29(59)53-37(25-30-13-4-2-5-14-30)42(61)55-36-20-11-22-50-41(60)35(19-10-23-51-47(48)49)54-44(63)39(27-32-28-52-34-18-9-8-17-33(32)34)56-43(62)38(26-31-15-6-3-7-16-31)57-45(64)40-21-12-24-58(40)46(36)65/h2,4-5,8-9,13-14,17-18,28,31,35-40,52H,3,6-7,10-12,15-16,19-27H2,1H3,(H,50,60)(H,53,59)(H,54,63)(H,55,61)(H,56,62)(H,57,64)(H4,48,49,51)/t35-,36-,37-,38+,39-,40-/m0/s1
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| Chemical Name |
(S)-N-((3R,6S,9S,15S,20aS)-6-((1H-indol-3-yl)methyl)-3-(cyclohexylmethyl)-9-(3-guanidinopropyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl)-2-acetamido-3-phenylpropanamide
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| Synonyms |
PMX 53 PMX 53 PMX53
Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)
AcPhe(ornithine-Pro-cyclohexylamine-Trp-Arg.
AcPhe(ornithine-Pro-cyclohexylamine-Trp-Arg)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~223.19 mM)
H2O : ~2.5 mg/mL (~2.79 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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