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Reltecimod (NSC-37096; AB-103; P-2TA) is a novel and potent CD28 antigen inhibitor with the potential for the treatment of necrotizing soft tissue infection. As a T-cell-specific surface glycoprotein CD28 (TP44) antagonist, Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it.
| 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 |
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| References |
[1]. Shirvan, A., et al. Reltecimod. T-cell-specific surface glycoprotein CD28 (TP44) antagonist, CD28 homodimer interface mimetic peptide, Treatment of necrotizing soft-tissue infection. Drugs Fut 2018, 43(4): 243
[2]. Edgar, R., Tarrio, M.L., Maislin, G. et al. Treatment with One Dose of Reltecimod is Superior to Two Doses in Mouse Models of Lethal Infection. Int J Pept Res Ther 26, 1669–1683 (2020). |
| Molecular Formula |
C46H72N10O15S
|
|---|---|
| Molecular Weight |
1037.197
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| Exact Mass |
1036.4899
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| CAS # |
1447799-33-8
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| Related CAS # |
Reltecimod TFA
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(O)C[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H]1N(C([C@H](CO)NC([C@@H](C)N)=O)=O)CCC1)=O)CCSC)=O)CC(C)C)=O)C(C)C)=O)C)=O)CC2=CC=C(O)C=C2)=O)C(N[C@@H](C(O)=O)C)=O
|
| 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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| 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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