| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
DMT1 blocker 1 targets divalent metal transporter 1 (DMT1), also known as SLC11A2 or NRAMP2. DMT1 is a transmembrane protein that mediates the transport of divalent metals, particularly iron (Fe²⁺), across cellular membranes. It plays a critical role in intestinal iron absorption and cellular iron uptake. By blocking DMT1, the compound inhibits iron transport and reduces cellular iron accumulation. The compound has an IC₅₀ of 0.64 μM for DMT1 inhibition.
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| ln Vitro |
In vitro, DMT1 blocker 1 potently inhibits DMT1-mediated iron transport with an IC₅₀ of 0.64 μM. The compound effectively reduces iron absorption and intracellular accumulation in cell-based assays. It is expected to block the absorption of iron by intestinal cells. The compound's activity is assessed by measuring iron uptake in DMT1-expressing cells. No other in vitro activities have been reported for DMT1 blocker 1.
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| ln Vivo |
In vivo, DMT1 blocker 1 is expected to block the absorption of iron by intestinal cells. By blocking DMT1 activity, the compound may reduce systemic iron levels and prevent iron overload. It is widely used in studies of iron metabolism, neurodegenerative diseases, and anemia. However, specific in vivo efficacy data have not been extensively reported. Further studies are needed to evaluate its effects in animal models.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for DMT1 blocker 1 typically involve measuring inhibition of DMT1-mediated iron transport. DMT1-expressing cells (e.g., HEK293 cells transfected with DMT1) are cultured and treated with various concentrations of the compound. Iron uptake is measured using radiolabeled iron (⁵⁵Fe or ⁵⁹Fe) or fluorescent iron indicators. Cells are incubated with the compound and iron for a specific period, and intracellular iron content is quantified. IC₅₀ values are determined from concentration-response curves.
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| Cell Assay |
In vitro cell-based assays for DMT1 blocker 1 typically employ DMT1-expressing cell lines such as HEK293, Caco-2 (intestinal epithelial cells), or other relevant cell types. Cells are cultured in appropriate medium and treated with various concentrations of the compound (typically 0.1-10 μM). Iron uptake is measured using radiolabeled iron or fluorescent probes. Cellular iron content is quantified by atomic absorption spectroscopy or colorimetric assays. Cell viability is assessed to ensure that the observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo animal studies with DMT1 blocker 1 have not been extensively reported. The compound is expected to block iron absorption in the intestine. However, specific animal studies evaluating its pharmacokinetics, efficacy, or toxicology have not been described. Future studies may involve oral administration of the compound to rodents to evaluate its effects on iron absorption and systemic iron levels. Currently, limited in vivo data are available.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of DMT1 blocker 1 have not been characterized. No absorption, distribution, metabolism, or excretion studies have been conducted. As a small molecule with a molecular weight of 294.31, the compound may have reasonable oral bioavailability and cell permeability. However, these properties have not been experimentally determined. Further studies are needed to evaluate the compound's PK profile.
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| Toxicity/Toxicokinetics |
The toxicity profile of DMT1 blocker 1 has not been characterized in preclinical studies. No acute toxicity, genotoxicity, or chronic toxicity studies have been reported. The compound is intended for research use only and is not approved for human therapeutic applications. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
DMT1 blocker 1 is a research-grade small-molecule blocker of divalent metal transporter 1 (DMT1). It has a molecular formula of C₁₆H₁₄N₄O₂ and a molecular weight of 294.31. The compound has an IC₅₀ of 0.64 μM for DMT1 inhibition. By blocking DMT1 activity, it reduces iron absorption and intracellular accumulation. It is widely used in studies of iron metabolism, neurodegenerative diseases, and anemia. The compound is not an approved therapeutic drug and has no clinical trial history. It is supplied as a high-purity powder (≥99%) and should be stored appropriately.
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| Molecular Formula |
C16H14N4O2
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|---|---|
| Molecular Weight |
294.30796289444
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| Exact Mass |
294.111
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| CAS # |
1354790-56-9
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| PubChem CID |
25098135
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| Appearance |
White to pink solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
483
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(=O)N(N1)C2=CC=CC=N2)C(=O)NC3=CC=CC=C3
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| InChi Key |
QJEBTCLOCMTSJU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N4O2/c1-11-14(15(21)18-12-7-3-2-4-8-12)16(22)20(19-11)13-9-5-6-10-17-13/h2-10,19H,1H3,(H,18,21)
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| Chemical Name |
5-methyl-3-oxo-N-phenyl-2-pyridin-2-yl-1H-pyrazole-4-carboxamide
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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) |
DMSO : ~50 mg/mL (~169.89 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.82 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (2.82 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 8.3 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: ≥ 0.83 mg/mL (2.82 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 | 3.3978 mL | 16.9889 mL | 33.9778 mL | |
| 5 mM | 0.6796 mL | 3.3978 mL | 6.7956 mL | |
| 10 mM | 0.3398 mL | 1.6989 mL | 3.3978 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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