| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
CXCR2 (CXC chemokine receptor 2).
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|---|---|
| ln Vitro |
In the conditioned media of human lung epithelial cells (A549) activated with TNF-α (20 ng/mL) or IL-1β (10 ng/mL), there is a powerful PMN chemokine called peptide 78. With 78 amino acids and an 8.3 kDa molecular weight, peptide 78 shares four cysteines with IL-8 and its homologs. Platelet factor 4, platelet basic protein, and the products of its cleavage (connective tissue activating peptide-III, β-thromboglobulin and interferon-γ-induced protein, macrophage inflammatory protein-2α, and macrophage inflammatory protein-2α) are among the supergene family of which peptide 78 is a member. Inflammatory protein-2β) phagocytosis) [1]. Peptide 78, like NAP-2 or LL-8, possesses a number of PMN-activating characteristics. Peptide 78 stimulated PMNs in a way that resulted in considerable chemotactic activity, the release of free cytosolic calcium, and the release of elastase from cells that had been pretreated with cytochalasin B. PMN recruitment to RA-inflamed joints is aided by peptide 78. One of the most prevalent chemokines found in RA synovial fluid is peptide 78. The physiologically active peptide 78 is found in rheumatoid arthritis synovial fluid. About half of the RA synovial fluid PMN's in vitro chemotactic activity appears to be accounted for by peptide 78 [1].
Peptide 78 is a definitive CXCR2-exclusive agonist with no CXCR1 cross-reactivity. It is 90-fold elevated in RA versus osteoarthritis synovial fluid. Anti-ENA-78 antibodies reduce RA chemotactic activity by 42%. N-terminal variants achieve up to 8-fold higher chemotactic potency. Unlike IL-8 and GCP-2, Peptide 78 fails to suppress TNF-α-induced oxidant production. |
| ln Vivo |
Peptide 78 is one of the most abundant chemokines present in RA synovial fluid and is biologically active. It induces neutrophil chemotaxis and plays an important role in rheumatoid arthritis joints. The peptide represents a key mediator of neutrophil recruitment in inflammatory conditions.
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| Enzyme Assay |
In vitro receptor binding assays measure the affinity of Peptide 78 for CXCR2 using membrane preparations from cells expressing recombinant human CXCR2. Radiolabeled Peptide 78 (e.g., 125I-labeled) is incubated with membranes and varying concentrations of unlabeled peptide. Bound and free radioactivity are separated by filtration. Ki values are calculated from competition binding curves. Selectivity is confirmed by lack of binding to CXCR1.
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| Cell Assay |
In vitro cellular chemotaxis assays use primary human neutrophils or CXCR2-expressing cell lines. Cells are placed in the upper chamber of a Transwell plate. Peptide 78 is added to the lower chamber at concentrations ranging from 0.1-100 nM. Migrated cells are counted after 1-2 hours. Calcium flux is measured using fluorescent dyes (e.g., Fluo-4) following peptide stimulation. Receptor internalization is assessed by flow cytometry.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse models of rheumatoid arthritis or acute inflammation. Peptide 78 is administered locally (intra-articular or intraperitoneal) or systemically. Neutrophil recruitment is assessed by measuring myeloperoxidase activity in tissues or by flow cytometry of bronchoalveolar lavage fluid. Inflammatory cytokine levels are measured by ELISA. Joint swelling and histological scoring are performed in arthritis models.
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| ADME/Pharmacokinetics |
Peptide 78 (CXCL5) has a molecular weight of 1542.7 g/mol and molecular formula C62H107N23O21S. CAS number: 132116-62-2. Store as a lyophilized powder at -20°C. Reconstitute in sterile water or buffer. For in vivo use, formulate in sterile saline or PBS. The peptide is stable for up to 1 year when stored desiccated at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for Peptide 78. As a research peptide, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments would include evaluation of cytokine release syndrome potential, immunogenicity, and off-target chemokine receptor activation. The peptide is for research use only.
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| References | |
| Additional Infomation |
Peptide 78 is a research-grade CXCR2-selective chemokine for studying neutrophil biology and inflammation. It is not approved for clinical use. Also known as ENA-78 and CXCL5. The peptide sequence includes 78 amino acids. It is supplied as a lyophilized powder with high purity and should be stored desiccated at -20°C. It is a valuable tool for studying rheumatoid arthritis and neutrophil recruitment.
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| Molecular Formula |
C60H106N22O20S
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|---|---|
| Molecular Weight |
1487.7
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| Exact Mass |
1541.773
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| CAS # |
132116-62-2
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| PubChem CID |
3081257
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.685
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| LogP |
-5.09
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
107
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| Complexity |
3200
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| Defined Atom Stereocenter Count |
14
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(=O)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)N)C(=O)O)N)O
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| InChi Key |
BNIFSVVAHBLNTN-XKKUQSFHSA-N
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| InChi Code |
InChI=1S/C62H107N23O21S/c1-29(2)47(57(102)74-30(3)48(93)81-38(60(105)106)25-43(65)89)83-53(98)36(26-45(91)92)80-55(100)41-16-11-22-85(41)59(104)37(24-42(64)88)75-44(90)27-73-49(94)39(28-86)82-51(96)33(14-9-20-72-62(69)70)77-54(99)40-15-10-21-84(40)58(103)35(12-6-7-18-63)79-50(95)32(13-8-19-71-61(67)68)76-52(97)34(17-23-107-5)78-56(101)46(66)31(4)87/h29-41,46-47,86-87H,6-28,63,66H2,1-5H3,(H2,64,88)(H2,65,89)(H,73,94)(H,74,102)(H,75,90)(H,76,97)(H,77,99)(H,78,101)(H,79,95)(H,80,100)(H,81,93)(H,82,96)(H,83,98)(H,91,92)(H,105,106)(H4,67,68,71)(H4,69,70,72)/t30-,31+,32-,33-,34-,35-,36-,37-,38-,39-,40-,41-,46-,47-/m0/s1
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| Chemical Name |
(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-4-oxobutanoic acid
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| Synonyms |
Peptide78; Peptide-78; Peptide 78
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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, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~64.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (64.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6722 mL | 3.3609 mL | 6.7218 mL | |
| 5 mM | 0.1344 mL | 0.6722 mL | 1.3444 mL | |
| 10 mM | 0.0672 mL | 0.3361 mL | 0.6722 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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