| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
Bioactive penta-peptide
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|---|---|
| ln Vitro |
- Enhancement of T-cell lineage generation：Thymopentin (10–100 nM) significantly increases the proportion of CD3⁺, CD4⁺, and CD8⁺ T cells derived from human embryonic stem cells (hESCs) in vitro. Flow cytometry analysis shows a 2- to 3-fold increase in T-cell markers compared to untreated controls. [1]
- Upregulation of T-cell differentiation genes：Quantitative PCR reveals that Thymopentin treatment upregulates the expression of T-cell-specific transcription factors (e.g., TCF7, GATA3) by 1.5–2.0-fold in hESC-derived hematopoietic progenitor cells. [1] Thymopentin acetate promotes T cell lineages generated from human embryonic stem cells in vitro [1]. |
| ln Vivo |
- Enhanced immune response in mice：Subcutaneous administration of Thymopentin (0.1–1 mg/kg) in BALB/c mice increases splenic T-cell proliferation by 40–60% (measured via BrdU incorporation) and elevates serum interferon-γ levels by 2-fold. [2]
- Improved skin permeation via microneedles：In a rat skin model, dissolving microneedle arrays encapsulating Thymopentin achieve 80–90% drug release within 30 minutes, with a skin penetration efficiency 5-fold higher than conventional topical administration. [2] |
| Cell Assay |
- T-cell differentiation assay：
1. hESCs are induced to differentiate into hematopoietic progenitor cells in serum-free medium supplemented with cytokines (e.g., SCF, IL-3).
2. Thymopentin (10–100 nM) is added during the T-cell specification phase.
3. After 14 days, cells are stained with anti-CD3, CD4, and CD8 antibodies and analyzed by flow cytometry. [1]
- Microneedle drug release assay： 1. Dissolving microneedle arrays loaded with Thymopentin are incubated in phosphate-buffered saline (pH 7.4) at 37°C. 2. Drug release is monitored using HPLC, with cumulative release measured at 15, 30, 60, and 120 minutes. [2] |
| Animal Protocol |
- Immunomodulation study in mice：
1. BALB/c mice (6–8 weeks old) receive subcutaneous injections of Thymopentin (0.1–1 mg/kg) dissolved in saline every other day for 2 weeks.
2. Splenocytes are isolated and stimulated with concanavalin A to assess T-cell proliferation.
3. Serum cytokine levels are measured by ELISA. [2]
- Skin permeation study in rats： 1. Sprague-Dawley rats are anesthetized, and dissolving microneedle arrays containing Thymopentin are applied to the dorsal skin for 30 minutes. 2. Skin samples and plasma are collected at various time points to quantify drug levels via HPLC. [2] |
| ADME/Pharmacokinetics |
- Rapid absorption via microneedles：In rats, Thymopentin administered via microneedles reaches peak plasma concentrations (Cmax) of 20–30 ng/mL within 1 hour, with a half-life of 2–3 hours. [2]
- High skin retention：Approximately 30–40% of the administered dose remains in the skin tissue 24 hours post-application, indicating sustained local delivery. [2] |
| Toxicity/Toxicokinetics |
- No significant systemic toxicity：In mice, single doses of Thymopentin up to 10 mg/kg (microneedle administration) show no signs of acute toxicity, with normal liver and kidney function markers. [2]
- Local skin tolerance：Histological analysis of rat skin treated with microneedle arrays reveals minimal inflammation and no epidermal damage. [2] |
| References |
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| Additional Infomation |
- Mechanism of action：Thymopentin promotes T-cell differentiation by activating Notch signaling and upregulating T-cell lineage-specific genes in hESCs. [1]
- Novel delivery system：The dissolving microneedle array enhances transdermal delivery of Thymopentin, overcoming the low bioavailability of traditional subcutaneous injections. [2] - Therapeutic potential：Investigated for immune restoration in immunocompromised conditions and as an adjuvant for cancer immunotherapy. [1][2] |
| Molecular Formula |
C32H53N9O11
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|---|---|
| Molecular Weight |
739.816927671433
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| Exact Mass |
739.386
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| CAS # |
89318-88-7
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| Related CAS # |
Thymopentin;69558-55-0
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| PubChem CID |
53230082
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| Appearance |
White to off-white solid powder
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| LogP |
3.852
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
52
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| Complexity |
1140
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)N.CC(=O)O
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| InChi Key |
YRTISBKUCLDRGF-ADVSENJOSA-N
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| InChi Code |
InChI=1S/C30H49N9O9.C2H4O2/c1-16(2)24(28(46)38-22(29(47)48)14-17-8-10-18(40)11-9-17)39-27(45)21(15-23(41)42)37-26(44)20(7-3-4-12-31)36-25(43)19(32)6-5-13-35-30(33)34;1-2(3)4/h8-11,16,19-22,24,40H,3-7,12-15,31-32H2,1-2H3,(H,36,43)(H,37,44)(H,38,46)(H,39,45)(H,41,42)(H,47,48)(H4,33,34,35);1H3,(H,3,4)/t19-,20-,21-,22-,24-;/m0./s1
|
| Chemical Name |
acetic acid;(3S)-3-[[(2S)-6-amino-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-4-[[(2S)-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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| Synonyms |
Thymopentin monoacetate; 89318-88-7; UNII-1938Y8P51M; DTXSID80237615; 1938Y8P51M; L-Tyrosine, L-arginyl-L-lysyl-L-alpha-aspartyl-L-valyl-, monoacetate (Salt); L-Tyrosine, N-(N-(N-(n2-L-arginyl-L-lysyl)-L-alpha-aspartyl)-L-valyl)-, monoacetate; DTXCID30160106;
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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 : ~25 mg/mL (~33.79 mM)
DMSO : ~25 mg/mL (~33.79 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (2.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (2.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (2.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3517 mL | 6.7584 mL | 13.5168 mL | |
| 5 mM | 0.2703 mL | 1.3517 mL | 2.7034 mL | |
| 10 mM | 0.1352 mL | 0.6758 mL | 1.3517 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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