| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Targets |
CD28 (T-cell-specific surface glycoprotein / TP44). CD28 is a critical co-stimulatory receptor on T cells that provides essential signals for T-cell activation, proliferation, and survival. By antagonizing CD28, Reltecimod modulates T-cell co-stimulatory signaling and downstream effects of CD28 pathway engagement.
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|---|---|
| ln Vitro |
In vitro, Reltecimod functions as a CD28 antagonist, modulating T-cell co-stimulatory signaling. The peptide serves as a robust probe for investigating T-cell co-stimulatory signaling and the downstream effects of CD28 pathway engagement. Its immunomodulatory activity has been characterized in various in vitro assays using primary human T cells and T-cell lines.
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| ln Vivo |
In vivo, Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. The compound has been studied in animal models of necrotizing soft-tissue infections (NSTIs). Its ability to modulate T-cell responses without completely eliminating immune function makes it a promising immunomodulatory agent for infectious and inflammatory conditions.
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| Enzyme Assay |
Cell-free assays for Reltecimod are limited due to its nature as a peptide immunomodulator. Binding studies to CD28 can be performed using surface plasmon resonance (SPR) or ELISA-based binding assays with immobilized recombinant human CD28 protein. The peptide is incubated with CD28 at varying concentrations, and binding affinity is determined. Competition assays with labeled CD80 or CD86 (the natural ligands of CD28) can be performed to assess the peptide's ability to block CD28-ligand interactions.
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| Cell Assay |
Cellular assays for Reltecimod use primary human T cells or T-cell lines (e.g., Jurkat cells) stimulated with anti-CD3 and anti-CD28 antibodies or with antigen-presenting cells expressing CD80/CD86. Cells are treated with Reltecimod at concentrations ranging from 0.01-100 μM for 24-72 hours. T-cell activation is measured by assessing proliferation (via [³H]-thymidine incorporation or CFSE dilution), cytokine production (IL-2, IFN-γ, TNF-α by ELISA or flow cytometry), and expression of activation markers (CD25, CD69 by flow cytometry). Inhibition of CD28-mediated co-stimulation is calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Pathogen-free, female balb/c (Bagg ALBino) mouse (acute bacterial peritonitis induced by intraperitoneal (ip) injection of E. coli). Reltecimod (1.25-5 mg/kg; iv) can improve the survival rate of mice infected with different bacteria [2]. E. coli 018:K1)[2]
Doses: 1.25 or 5 mg/kg Route of Administration: IV; single dose; 4 hrs (hrs (hours)) post-infection Experimental Results: 100% survival on day 6, single dose of 5 mg/kg . Survival rate was 70% at 4 doses (1, 12, 24 and 36 hrs (hrs (hours)) post-infection) of 1.25 mg/kg Animal/Disease Models: Pathogen-free female balb/c (Bagg ALBino) mouse (NSTI induced by intramuscularinjection of Streptococcus pyogenes into the thigh) [ 2] Doses: 2.5 or 5 mg/kg as a single dose; 1 hour, or 1 hour, 12 hrs (hrs (hours)), or 72 hrs (hrs (hours)) after infection. Experimental Results: Day 8, single dose of 2.5 mg/kg resulted in 65% survival. Survival rate was 30% after two doses (1 hour and 12 hrs (hrs (hours)) post-infection) of 2.5 mg/kg on day 8. A single dose (1 hour after infection) of 5 mg/kg resulted in a survival rate of 90% on day 6. Animal/Disease Models: Pathogen-free femal In vivo efficacy studies are conducted in mouse models of bacterial infection or necrotizing soft-tissue infections. Reltecimod is administered via intravenous or intraperitoneal injection at doses typically ranging from 1-30 mg/kg. Disease progression is monitored by measuring bacterial load, survival, and assessment of tissue damage. In models of radiation exposure, survival and hematopoietic recovery are assessed. Immunological endpoints include measurement of T-cell activation markers and cytokine levels in plasma and tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of Reltecimod as a peptide are limited. As a peptide therapeutic, the compound is administered parenterally and is subject to proteolytic degradation. Its half-life is determined by its stability in plasma and tissues. PK parameters such as Cmax, Tmax, AUC, and half-life are determined in preclinical species. The compound's distribution is primarily to the vascular compartment and tissues with high blood flow. Metabolism occurs via peptidase-mediated degradation.
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| Toxicity/Toxicokinetics |
Toxicological data for Reltecimod are limited to preclinical studies. As a CD28 antagonist, potential toxicities may include immunosuppression and increased susceptibility to infections. The compound's immunomodulatory effects are expected to be reversible upon drug discontinuation. Standard toxicology studies would be required for clinical development. At research-grade doses, the compound is handled with standard laboratory precautions. Comprehensive safety data are not widely reported in public sources.
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| References |
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| Additional Infomation |
Reltecimod is being investigated in the clinical trial NCT02469857 (Phase III efficacy and safety study of AB103 in patients with necrotizing soft tissue infection).
Reltecimod (AB-103) is a research compound being developed for the treatment of necrotizing soft-tissue infections and other conditions involving dysregulated T-cell responses. It is not an approved therapeutic agent. The compound is available from chemical suppliers for research purposes only. Its mechanism as a CD28 antagonist makes it a valuable tool for studying T-cell co-stimulation and for developing immunomodulatory therapies. The peptide is typically stored lyophilized at -20°C and reconstituted in appropriate buffers for experimental use. |
| Molecular Formula |
C46H72N10O15S
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|---|---|
| Molecular Weight |
1037.197
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| Exact Mass |
1036.489
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| CAS # |
1447799-33-8
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| Related CAS # |
Reltecimod TFA
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| PubChem CID |
71652162
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1473.8±65.0 °C at 760 mmHg
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| Flash Point |
845.1±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
1.38
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
72
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| Complexity |
1920
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C[C@H](C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C)C(=O)O)N
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| InChi Key |
VRNHFZYMPDKTBS-WYUJEMNCSA-N
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| InChi Code |
InChI=1S/C46H72N10O15S/c1-22(2)18-30(52-39(63)29(15-17-72-8)50-43(67)34-10-9-16-56(34)45(69)33(21-57)54-37(61)24(5)47)42(66)55-36(23(3)4)44(68)48-25(6)38(62)51-31(19-27-11-13-28(58)14-12-27)41(65)53-32(20-35(59)60)40(64)49-26(7)46(70)71/h11-14,22-26,29-34,36,57-58H,9-10,15-21,47H2,1-8H3,(H,48,68)(H,49,64)(H,50,67)(H,51,62)(H,52,63)(H,53,65)(H,54,61)(H,55,66)(H,59,60)(H,70,71)/t24-,25+,26-,29+,30+,31+,32+,33+,34+,36+/m1/s1
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| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2R)-2-aminopropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-[[(1R)-1-carboxyethyl]amino]-4-oxobutanoic acid
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| Synonyms |
Reltecimod AB103 NSC37096P-2TA NSC-37096AB-103 P2TA NSC37096 BENZCARBIMINE.
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9641 mL | 4.8207 mL | 9.6413 mL | |
| 5 mM | 0.1928 mL | 0.9641 mL | 1.9283 mL | |
| 10 mM | 0.0964 mL | 0.4821 mL | 0.9641 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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