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| Targets |
PLP 139-151 targets the immune system, specifically T cells that recognize this myelin epitope. The peptide corresponds to amino acid residues 139 to 151 of myelin proteolipid protein (PLP). When administered to susceptible mouse strains (such as SJL/J mice) in the presence of adjuvants, PLP 139-151 activates autoreactive T cells that recognize the PLP epitope. These activated T cells cross the blood-brain barrier and initiate an inflammatory response against central nervous system myelin, leading to demyelination and clinical signs of EAE. The peptide is presented by MHC class II molecules (particularly I-A^s in SJL/J mice) to CD4+ T cells. The resulting immune response mimics the autoimmune attack on myelin that occurs in multiple sclerosis. PLP 139-151 is one of the most well-characterized encephalitogenic peptides used in EAE research.
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| ln Vitro |
Adoptive transfer of peptide-specific T cell lines and 3 of 4 T cell clones generated severe clinical and histological EAE. In in vitro proliferation experiments, T cell lines/clones responded strongly to PLP (139-151). The SPL line and its clones demonstrated a robust proliferative response to the whole PLP molecule and PLP (139-151) [1].
In vitro, PLP 139-151 is used to stimulate T cell responses in proliferation and cytokine production assays. T cells from immunized animals or from patients with multiple sclerosis can be restimulated in vitro with PLP 139-151 to assess their reactivity to the myelin epitope. T cell proliferation is measured by [3H]-thymidine incorporation or CFSE dilution following peptide stimulation. Cytokine production (IFN-gamma, IL-17, IL-4, IL-10) is measured by ELISA or ELISpot following peptide stimulation. The peptide's ability to activate T cells in vitro is concentration-dependent, with optimal stimulation typically observed at concentrations of 10-50 microg/mL. The peptide is also used in MHC class II binding assays to study the interaction between PLP 139-151 and MHC molecules. These in vitro assays are essential for characterizing the immune response to PLP and for evaluating potential immunomodulatory therapies. |
| ln Vivo |
PLP (139–151) can be utilized to create autoimmune brain blockage models in animals.
In vivo, PLP 139-151 is used to induce experimental autoimmune encephalomyelitis (EAE) in susceptible mouse strains. The peptide is typically emulsified in complete Freund's adjuvant (CFA) containing heat-killed Mycobacterium tuberculosis and administered by subcutaneous injection. Pertussis toxin is often administered intravenously on the day of immunization and two days later to enhance disease induction. Clinical signs of EAE typically appear 10-14 days after immunization and follow a relapsing-remitting course in SJL/J mice, characterized by ascending paralysis starting with tail weakness and progressing to hind limb and forelimb paralysis. Disease severity is scored using a standard clinical scale (0-5). The PLP 139-151-induced EAE model is one of the most widely used models for studying multiple sclerosis and evaluating potential therapies. |
| Enzyme Assay |
In vitro assays for PLP 139-151 typically involve T cell proliferation and cytokine production assays. For proliferation assays, lymphocytes (splenocytes or lymph node cells) from PLP 139-151-immunized mice are cultured in 96-well plates with varying concentrations of the peptide (typically 0.1-100 microg/mL). After 48-72 hours of culture, [3H]-thymidine is added, and incorporation is measured after an additional 16-24 hours. Alternatively, CFSE labeling can be used to track cell division by flow cytometry. For cytokine production assays, cell culture supernatants are collected after 48-72 hours of peptide stimulation, and cytokine levels (IFN-gamma, IL-17, IL-4, IL-10, etc.) are measured by ELISA or multiplex bead-based assays. ELISpot assays can be used to quantify the number of cytokine-producing cells. MHC class II binding assays can be performed using purified MHC molecules and labeled peptide.
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| Cell Assay |
In vitro cellular assays for PLP 139-151 are performed using primary lymphocytes from immunized animals or from patients with multiple sclerosis. Splenocytes or lymph node cells are isolated from PLP 139-151-immunized mice and cultured in complete medium. Cells are stimulated with varying concentrations of PLP 139-151 (typically 1-50 microg/mL) for 48-96 hours. T cell proliferation is measured by [3H]-thymidine incorporation or CFSE dilution. Cytokine production is measured by ELISA or ELISpot. For human studies, peripheral blood mononuclear cells (PBMCs) from MS patients or healthy controls are stimulated with PLP 139-151, and T cell responses are measured similarly. Cytotoxicity is assessed using standard viability assays to ensure that observed responses are not due to cell death. The specificity of the response is confirmed by using unrelated control peptides.
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| Animal Protocol |
In vivo animal studies for PLP 139-151 are conducted to induce EAE and to evaluate potential therapies. Female SJL/J mice (6-8 weeks old) are the most commonly used strain. Mice are immunized subcutaneously with 100-200 microg of PLP 139-151 emulsified in complete Freund's adjuvant (CFA) containing 400-500 microg of heat-killed Mycobacterium tuberculosis. Pertussis toxin (200-400 ng) is administered intravenously on the day of immunization and two days later. Clinical signs are scored daily using a 0-5 scale: 0 = no signs, 1 = limp tail, 2 = hind limb weakness, 3 = hind limb paralysis, 4 = forelimb weakness, 5 = moribund or dead. Disease typically follows a relapsing-remitting course. At study termination, spinal cords and brains are collected for histopathological examination to assess demyelination and inflammation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PLP 139-151 are characteristic of a peptide administered for immunization purposes. The peptide has a molecular formula of C72H104N20O16S and a molecular weight of 1537.79 g/mol. PLP 139-151 is soluble in water at 90 mg/mL. When administered in complete Freund's adjuvant, the peptide is slowly released from the emulsion, providing sustained antigen exposure for immune activation. The peptide is not typically administered as a therapeutic agent but rather as an immunogen to induce EAE. Comprehensive pharmacokinetic studies on the absorption, distribution, metabolism, and elimination of PLP 139-151 have not been extensively reported, as the peptide is used as a research tool rather than a therapeutic candidate.
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| Toxicity/Toxicokinetics |
PLP 139-151 is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a peptide derived from a self-protein (myelin proteolipid protein), the compound is immunogenic and can induce autoimmune disease when administered in adjuvant. This is the intended effect for EAE induction, not a toxicological concern. However, the peptide itself is not toxic at the concentrations used for immunization. Standard in vitro cytotoxicity assays in cell lines are typically performed to rule out nonspecific toxicity. In vivo, animals immunized with PLP 139-151 are monitored for clinical signs of EAE and general health. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been reported for PLP 139-151. The peptide is not approved for human use and is strictly intended for research purposes.
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| References |
[1]. Kuchroo VK, et al. Induction of experimental allergic encephalomyelitis by myelin proteolipid-protein-specific T cell clones and synthetic peptides. Pathobiology. 1991;59(5):305-12.
[2]. Sobel RA, et al. Acute experimental allergic encephalomyelitis in SJL/J mice induced by a synthetic peptide ofmyelin proteolipid protein. J Neuropathol Exp Neurol. 1990 Sep;49(5):468-79. [3]. Bebo BF Jr, et al. Male SJL mice do not relapse after induction of EAE with PLP 139-151. J Neurosci Res. 1996 Sep 15;45(6):680-9. |
| Additional Infomation |
PLP 139-151 is a synthetic peptide corresponding to amino acid residues 139 to 151 of myelin proteolipid protein (PLP). It is widely used to induce relapsing-remitting experimental autoimmune encephalomyelitis (RR-EAE) in SJL/J mice, a well-established animal model of multiple sclerosis. The peptide has a molecular formula of C72H104N20O16S and a molecular weight of 1537.79 g/mol. PLP 139-151 activates autoreactive T cells that recognize the PLP epitope, leading to an autoimmune attack on central nervous system myelin. The peptide is also used in vitro to study T cell responses to myelin antigens. PLP 139-151 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. PLP 139-151 is a valuable research tool for studying the immunopathogenesis of multiple sclerosis and evaluating potential therapeutic interventions.
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| Molecular Formula |
C72H104N20O16S
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| Molecular Weight |
1537.7856
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| Exact Mass |
1536.77
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| CAS # |
131334-43-5
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| PubChem CID |
102601612
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.976
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| Hydrogen Bond Donor Count |
20
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
47
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| Heavy Atom Count |
109
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| Complexity |
3040
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| Defined Atom Stereocenter Count |
11
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| SMILES |
S([H])C([H])([H])[C@@]([H])(C(N([H])[C@]([H])(C(N([H])C([H])([H])C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)C(N([H])[C@]([H])(C(N([H])C([H])([H])C(N([H])[C@@]([H])(C([H])([H])C1=C([H])N=C([H])N1[H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)C([H])([H])C(=O)O[H])=O)=O)=O)=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C1=C([H])N=C([H])N1[H])N([H])[H])=O
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| InChi Key |
VTBYVGRYDXYLHZ-UVIWMAFZSA-N
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| InChi Code |
InChI=1S/C72H104N20O16S/c1-40(2)25-51(63(98)80-36-60(94)84-55(30-45-34-77-39-82-45)71(106)92-24-14-21-58(92)70(105)89-54(31-61(95)96)68(103)85-50(20-11-13-23-74)66(101)90-56(72(107)108)27-42-15-6-5-7-16-42)86-67(102)53(28-43-32-78-48-18-9-8-17-46(43)48)88-65(100)49(19-10-12-22-73)83-59(93)35-79-64(99)52(26-41(3)4)87-69(104)57(37-109)91-62(97)47(75)29-44-33-76-38-81-44/h5-9,15-18,32-34,38-41,47,49-58,78,109H,10-14,19-31,35-37,73-75H2,1-4H3,(H,76,81)(H,77,82)(H,79,99)(H,80,98)(H,83,93)(H,84,94)(H,85,103)(H,86,102)(H,87,104)(H,88,100)(H,89,105)(H,90,101)(H,91,97)(H,95,96)(H,107,108)/t47-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-/m0/s1
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| Chemical Name |
(3S)-3-[[(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-4-[[(2S)-6-amino-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid
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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 (~65.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (32.51 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 | 0.6503 mL | 3.2514 mL | 6.5028 mL | |
| 5 mM | 0.1301 mL | 0.6503 mL | 1.3006 mL | |
| 10 mM | 0.0650 mL | 0.3251 mL | 0.6503 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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