| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The primary target of TMPRSS6-IN-1 TFA is TMPRSS6 (Matriptase-2), a member of the type II transmembrane serine protease (TTSP) family. TMPRSS6 is a key negative regulator of hepcidin expression, which in turn controls systemic iron homeostasis by modulating iron absorption and recycling. Inhibition of TMPRSS6 activity leads to increased hepcidin levels, reduced iron absorption, and improved erythropoiesis in conditions of iron overload and beta-thalassemia.
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| ln Vitro |
TMPRSS6-IN-1 TFA is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to the TTSP family (transmembrane serine protease). The compound specifically targets the proteolytic activity of this type II transmembrane serine protease. While detailed IC50 values are not provided, the designation as a potent inhibitor indicates strong in vitro binding and inhibitory activity against the recombinant enzyme in cell-free assays.
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| ln Vivo |
Genetic reduction of TMPRSS6 levels improves symptoms of hemochromatosis and beta-thalassemia in mouse models. By inhibiting TMPRSS6, hepcidin expression is increased, which reduces dietary iron absorption and improves the anemia and ineffective erythropoiesis characteristic of beta-thalassemia. This makes TMPRSS6 inhibitors promising therapeutic candidates for iron overload disorders and beta-thalassemia.
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| Enzyme Assay |
Typical TMPRSS6 inhibition assay: Recombinant TMPRSS6 enzyme is incubated with a fluorogenic peptide substrate (e.g., Boc-QAR-AMC) in assay buffer (50 mM Tris-HCl pH 8.5, 150 mM NaCl, 1 mM EDTA, 0.01% Tween-20) at 37degC for 30 minutes. TMPRSS6-IN-1 TFA is added at varying concentrations (0.1-10,000 nM). The reaction is terminated by adding 1% trifluoroacetic acid. Fluorescence (Ex 360 nm/Em 460 nm) is measured, and the IC50 value is calculated.
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| Cell Assay |
No specific cell-based protocols for TMPRSS6-IN-1 TFA were found. A standard cellular assay for TMPRSS6 inhibition would use cells engineered to express TMPRSS6. Cells are treated with the compound (0.01-100 uM) for 24-72 hours. TMPRSS6 enzymatic activity is measured using a cell-permeable fluorogenic substrate (e.g., AMC-conjugated peptide). Hepcidin mRNA levels are quantified by qPCR. Western blot analysis of downstream signaling may also be performed.
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| Animal Protocol |
No specific animal protocol was found. A general protocol for evaluating TMPRSS6 inhibitors in vivo: 8-10 week old Hfe knockout mice (a model of hereditary hemochromatosis) or Hbbth3/+ mice (a beta-thalassemia model) are administered TMPRSS6-IN-1 TFA (e.g., 10-50 mg/kg, oral or IP) once daily for 14-28 days. Blood is collected for serum iron, transferrin saturation, and hepcidin measurements. Liver tissue is harvested for iron content analysis.
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| ADME/Pharmacokinetics |
No specific PK data was found for TMPRSS6-IN-1 TFA. As a small-molecule inhibitor, its pharmacokinetic properties would be assessed in standard preclinical studies. The compound is the TFA salt form, which typically improves solubility and stability. Standard PK would involve IV/oral administration in rodents followed by LC-MS/MS analysis of plasma concentrations to determine half-life, bioavailability, and clearance.
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| Toxicity/Toxicokinetics |
No toxicity data was found for TMPRSS6-IN-1 TFA. As a research compound, its safety profile has not been fully characterized. Based on its mechanism targeting TMPRSS6, a protease involved in iron regulation, potential toxicities might relate to unintended alterations in systemic iron homeostasis, leading to anemia or other iron-related disorders. Standard lab safety practices apply.
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| References | |
| Additional Infomation |
TMPRSS6-IN-1 TFA is a research-grade compound with molecular formula C35H41F3N8O6S2 and molecular weight 790.88. It is a TFA salt that is soluble in DMSO (125 mg/mL). The compound targets the TTSP family and is indicated for research into hemochromatosis and beta-thalassemia. For research use only, not for human therapeutic applications.
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| Molecular Formula |
C35H41F3N8O6S2
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| Molecular Weight |
790.88
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| Related CAS # |
TMPRSS6-IN-1;2088415-78-3
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| Appearance |
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 : ~125 mg/mL (~158.05 mM; with ultrasonication)
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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 | 1.2644 mL | 6.3221 mL | 12.6441 mL | |
| 5 mM | 0.2529 mL | 1.2644 mL | 2.5288 mL | |
| 10 mM | 0.1264 mL | 0.6322 mL | 1.2644 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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