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| Targets |
Angiotensin-Converting Enzyme (ACE). Ac-SDKP acts as a physiological modulator of ACE activity. Its biological effects, including inhibiting stem cell proliferation and reducing collagen deposition, are mediated by its ability to block the actions of a stem cell-specific proliferation stimulator and to interfere with the TGF-beta/Smad signaling pathway.
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| ln Vitro |
In vitro, Ac-SDKP acetate potently inhibits the entry of pluripotent hematopoietic stem cells into the S-phase of the cell cycle. It demonstrates anti-inflammatory effects by reducing the release of pro-inflammatory cytokines from immune cells. Its anti-fibrotic activity is evidenced by its ability to suppress the expression and activation of matrix metalloproteinases (MMPs) and to reduce collagen synthesis in cultured fibroblasts.
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| ln Vivo |
In vivo, Ac-SDKP acetate shows significant renoprotective effects in hypertensive mice by reducing albuminuria and glomerular injury. It also prevents left ventricular fibrosis and dysfunction in models of heart failure, confirming its anti-fibrotic efficacy. These effects are mediated by the inhibition of inflammatory cell infiltration and the suppression of collagen deposition in target organs.
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| Enzyme Assay |
Standard non-cellular assays for Ac-SDKP involve studying its interaction with purified ACE. Using a fluorometric or spectrophotometric assay, the kinetic parameters of its degradation are determined. Ac-SDKP is incubated with purified ACE in a suitable reaction buffer (e.g., Tris-HCl buffer with NaCl and ZnCl2). The reaction is quenched at specific time points, and the rate of formation of the degradation product (the tripeptide Ser-Asp-Lys-Pro) is quantified by HPLC. This assay confirms that Ac-SDKP is a specific substrate for the ACE N-terminal active site.
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| Cell Assay |
The in vitro cellular activity of Ac-SDKP can be assessed using cell cycle analysis on primary hematopoietic stem cells (HSCs) or on cardiac fibroblasts. For HSCs, lineage-negative (Lin-) cells are isolated from mouse bone marrow. They are cultured with Ac-SDKP acetate (e.g., 1 nM to 10 uM) in the presence of growth factors. After a defined period (e.g., 48-72 hours), the cells are pulsed with BrdU or EdU, and the percentage of cells in the S-phase is determined by flow cytometry. This quantifies the inhibition of HSC proliferation.
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| Animal Protocol |
The in vivo anti-fibrotic effect of Ac-SDKP is studied in an Angiotensin II (AngII)-induced hypertensive mouse model. Male C57BL/6J mice are infused with AngII (e.g., 1,000 ng/kg/min) using a subcutaneous osmotic minipump for 14 days. Ac-SDKP acetate is co-infused at a dose of 800 microg/kg/day. At the end of the study, the kidneys are harvested. One kidney is used for histological analysis (e.g., Masson's trichrome for collagen and PAS for glomerular matrix expansion). The other kidney is processed for Western blotting to assess markers of fibrosis (e.g., alpha-SMA, Collagen I, Fibronectin).
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| ADME/Pharmacokinetics |
The acetate salt of Ac-SDKP is more stable than the free peptide and is the form used in many in vivo studies. In rodents, Ac-SDKP is rapidly hydrolyzed by ACE, giving it a very short plasma half-life (t1/2) of approximately 4.5 minutes. It is cleared from the circulation almost entirely by ACE-mediated degradation, primarily by the N-domain. This short half-life is a key challenge for its therapeutic application.
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| Toxicity/Toxicokinetics |
The tetrapeptide Ac-SDKP is an endogenous biomolecule, and its acetate salt is generally considered safe at research doses. Comprehensive toxicology studies typical of drug development are not publicly available. However, because it inhibits hematopoietic stem cell proliferation, one potential on-target effect could be myelosuppression at very high or sustained doses. For research use, standard safety measures for peptides should be applied.
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| References | |
| Additional Infomation |
Ac-SDKP is a key endogenous regulator of the hematopoietic stem cell (HSC) niche, preventing the over-proliferation of stem cells. This regulatory role has generated interest in Ac-SDKP as a potential therapeutic agent or biomarker for diseases involving fibrosis, such as chronic kidney disease, cardiac hypertrophy, and scleroderma. It has not been approved for clinical use.
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| Molecular Formula |
C22H37N5O11
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| Molecular Weight |
547.56
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| Related CAS # |
N-Acetyl-Ser-Asp-Lys-Pro;127103-11-1;N-Acetyl-Ser-Asp-Lys-Pro TFA
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| Appearance |
White to off-white solid powder
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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) |
DMSO :~100 mg/mL (~182.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 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 25.0 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: ≥ 2.5 mg/mL (4.57 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 25.0 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: ≥ 2.5 mg/mL (4.57 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 | 1.8263 mL | 9.1314 mL | 18.2628 mL | |
| 5 mM | 0.3653 mL | 1.8263 mL | 3.6526 mL | |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8263 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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