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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Serum thymic factor acetate primarily targets immune cells and the neuroendocrine system, functioning as a zinc-dependent immunomodulator. It binds to specific receptors on T lymphocytes and other immune cells, promoting T-cell differentiation and maturation. It also acts on the pituitary gland as a hypophysiotropic factor, stimulating the release of various hormones including luteinizing hormone (LH), follicle-stimulating hormone (FSH), and growth hormone. Additionally, it inhibits ERK activation in renal tubular cells, providing protection against cephaloridine-induced nephrotoxicity. The compound indirectly modulates NF-kappaB signaling and inflammatory cytokine production through its effects on immune cell function .
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| ln Vitro |
In vitro studies demonstrate that Serum thymic factor acetate promotes T-cell differentiation and maturation in thymocyte cultures. It enhances the expression of T-cell surface markers (CD3, CD4, CD8) and increases IL-2 production in activated lymphocytes. In macrophage cultures, it reduces LPS-induced production of pro-inflammatory cytokines including TNF-alpha, IL-1beta, and IL-6 while promoting IL-10 secretion. At concentrations of 0.1-10 microg/mL, it protects primary rat renal tubular cells from cephaloridine-induced cytotoxicity by inhibiting ERK1/2 phosphorylation. No direct cytotoxicity is observed in various cell lines at concentrations up to 100 microg/mL .
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| ln Vivo |
In vivo studies have demonstrated that Serum thymic factor acetate exerts significant immunomodulatory and tissue-protective effects. In rats, intraperitoneal administration (50-200 microg/kg) protects against cephaloridine-induced nephrotoxicity via ERK inhibition, with significant reductions in serum creatinine and BUN levels. In mouse models of EMC-D virus-induced diabetes, administration prevents the development of diabetes and myocarditis. The compound exhibits analgesic activity in mouse pain models (writhing and hot plate tests) at doses of 100-300 microg/kg. Anti-diabetic effects are observed in streptozotocin-induced diabetic rats, with reduced blood glucose and improved insulin sensitivity .
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| Enzyme Assay |
For enzyme/receptor binding studies, a typical competitive binding assay is used with radiolabeled or fluorescently labeled Serum thymic factor. T-lymphocyte membranes (50-100 microg protein) are incubated with 0.5-5 nM [3H]-labeled compound in binding buffer (50 mM Tris-HCl, pH 7.4, containing 10 microM ZnCl2, 1 mM MgCl2, and 0.1% BSA) at 4degC for 2 hours. Non-specific binding is determined with 100-fold excess unlabeled compound. Bound and free ligand are separated by rapid filtration through GF/B glass fiber filters, followed by scintillation counting. Receptor binding affinity (Kd) is typically in the low nanomolar range in the presence of zinc .
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| Cell Assay |
For T-cell differentiation assays, human or murine thymocytes are isolated and cultured in RPMI-1640 medium supplemented with 10% FBS, 2 mM L-glutamine, 1 microM ZnCl2, and antibiotics. Cells are seeded at 1 × 10⁶ cells/mL in 24-well plates and treated with Serum thymic factor acetate (0.01-10 microg/mL) for 24-72 hours at 37degC in 5% CO2. T-cell maturation is assessed by flow cytometry using anti-CD3, anti-CD4, and anti-CD8 antibodies. Cytokine production is measured in culture supernatants by ELISA. For cytotoxicity protection assays, renal proximal tubular cells are incubated with compound (0.1-10 microg/mL) for 1 hour before cephaloridine challenge .
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| Animal Protocol |
In the rat cephaloridine-induced nephrotoxicity model, male Wistar rats (200-250 g) are pre-treated with Serum thymic factor acetate (50-200 microg/kg, intraperitoneally) once daily for 3 days. Cephaloridine (200 mg/kg, subcutaneous) is administered on day 3, 30 minutes after the final compound dose. Blood samples are collected at 24, 48, and 72 hours post-cephaloridine for serum creatinine and BUN measurement. Kidneys are harvested for histopathological examination and Western blot analysis of ERK phosphorylation. For diabetes studies, EMC-D virus is injected intraperitoneally into BALB/c mice, followed by compound administration (10-100 microg/kg/day) for 14 days. Blood glucose is monitored weekly .
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| ADME/Pharmacokinetics |
Pharmacokinetic studies in rodents show that Serum thymic factor acetate is rapidly absorbed after intraperitoneal administration with a Tmax of 15-30 minutes. Peak plasma concentrations are dose-dependent, with an elimination half-life of approximately 30-60 minutes due to rapid proteolytic degradation. Bioavailability after oral administration is very low (<5%) due to gastrointestinal peptide degradation. The compound distributes to lymphoid tissues, kidney, and to a lesser extent the brain. Plasma protein binding is approximately 60-70%. Metabolism occurs primarily via proteolysis in plasma and tissues, producing small peptide fragments and amino acids. Excretion is primarily renal, with >90% recovered as metabolites within 24 hours .
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| Toxicity/Toxicokinetics |
Acute toxicity studies in rodents report an intraperitoneal LD50 > 500 mg/kg, indicating low acute toxicity. Subchronic studies (28 days) with daily intraperitoneal doses up to 5 mg/kg show no significant adverse effects on body weight, organ weights, hematology, or serum chemistry parameters. No genotoxicity was observed in Ames tests or micronucleus assays. Reproductive toxicity studies at doses up to 2 mg/kg/day in pregnant rats showed no teratogenic effects, though embryo-fetal development studies are limited. At high doses (>10 mg/kg), mild injection site reactions and transient lethargy have been reported. The compound is generally well-tolerated in preclinical studies .
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| References |
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| Additional Infomation |
Serum thymic factor has been studied in clinical trials for various indications, including rheumatoid arthritis, primary immunodeficiencies, and aging-related immune decline, though the acetate salt form is primarily for research use. It has not received regulatory approval for human therapeutic use. The natural peptide (Thymulin) is known to be zinc-dependent, and serum levels decline with aging and in certain disease states. Ongoing research is exploring its potential in Alzheimer's disease, chronic inflammatory conditions, and metabolic disorders. The peptide is rapidly degraded in vivo, limiting its clinical development. Synthetic analogs with improved stability are under investigation. The compound exerts its effects through both immune modulation and direct neuroendocrine actions .
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| Molecular Formula |
C35H58N12O17
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| Molecular Weight |
918.91
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| Exact Mass |
918.404
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| CAS # |
125117-65-9
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| Related CAS # |
Serum thymic factor; 63958-90-7
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| PubChem CID |
172009759
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| Sequence |
{Pyr}-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn{Pyr}-AKSQGGSN
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| SequenceShortening |
{Pyr}-AKSQGGSN
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
16
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
64
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| Complexity |
1640
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)N)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)O)NC(=O)[C@@H]1CCC(=O)N1.CC(=O)O
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| InChi Key |
DRMRECIVHRVLDV-NUTCLOCMSA-N
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| InChi Code |
InChI=1S/C33H54N12O15.C2H4O2/c1-15(39-29(55)18-6-8-24(50)40-18)27(53)42-16(4-2-3-9-34)30(56)45-21(14-47)32(58)43-17(5-7-22(35)48)28(54)38-11-25(51)37-12-26(52)41-20(13-46)31(57)44-19(33(59)60)10-23(36)49;1-2(3)4/h15-21,46-47H,2-14,34H2,1H3,(H2,35,48)(H2,36,49)(H,37,51)(H,38,54)(H,39,55)(H,40,50)(H,41,52)(H,42,53)(H,43,58)(H,44,57)(H,45,56)(H,59,60);1H3,(H,3,4)/t15-,16-,17-,18-,19-,20-,21-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-4-amino-2-[[(2S)-2-[[2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]propanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid
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| Synonyms |
Thymulin acetate; Thymic factor acetate
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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 (108.82 mM)
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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 | 1.0882 mL | 5.4412 mL | 10.8825 mL | |
| 5 mM | 0.2176 mL | 1.0882 mL | 2.1765 mL | |
| 10 mM | 0.1088 mL | 0.5441 mL | 1.0882 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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