| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
The primary targets of 6-Formylpterin include xanthine oxidase (XO), reactive oxygen species (ROS) generation, and apoptosis pathways. It is an EC 1.17.3.2 (xanthine oxidase) inhibitor and a reactive oxygen species generator. It binds to one of two active sites on XO nearly quantitatively and irreversibly, preventing the metabolism of other substrates at the second site. The compound induces apoptosis in HL-60 cells and inhibits PanC-1 cell proliferation.
|
|---|---|
| ln Vitro |
6-Formylpterin (2 mM) causes HL-60 cells to create ROS [1]. 6- Formylpterin (0.5, 1, and 2 mM, 3 hours) causes HL-60 and Jurkat cells to have higher 2O2 concentration, which causes apoptosis [1].
In vitro, 6-Formylpterin (2 mM) produces ROS in HL-60 cells. It (0.5, 1, and 2 mM, 3 hours) increases H2O2 content in HL-60 and Jurkat cells, leading to apoptosis. The compound induces apoptosis in HL-60 cells and inhibits Fas-mediated apoptosis in Jurkat cells at 0.5 mM. It also inhibits PanC-1 cell proliferation. The compound demonstrates concentration-dependent effects on ROS generation and apoptosis. |
| ln Vivo |
In vivo activity of 6-Formylpterin has not been extensively characterized. As a xanthine oxidase inhibitor and folate metabolite, it has potential for studying purine metabolism and immune cell function. However, detailed in vivo pharmacokinetic and pharmacodynamic studies are limited. The compound is primarily studied for its in vitro activities.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for 6-Formylpterin typically involve xanthine oxidase inhibition studies. The enzyme is incubated with varying concentrations of the compound (0.1-100 µM) in appropriate buffer at 37°C. Xanthine oxidase activity is measured by monitoring the conversion of xanthine to uric acid using spectrophotometric methods. The compound demonstrates concentration-dependent inhibition of xanthine oxidase activity.
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: HL-60 cells, Jurkat cells Tested Concentrations: 0.5, 1, and 2 mM Incubation Duration: 3 h Experimental Results: Induced apoptosis in HL-60 cells[1]. Inhibited Fas-mediated apoptosis in Jurkat cells in 0.5 mM[1]. In vitro cellular assays for 6-Formylpterin involve testing its effects on ROS generation and apoptosis. HL-60 and Jurkat cells are treated with varying concentrations of 6-Formylpterin (0.5, 1, and 2 mM) for 3 hours. ROS production is measured using fluorescent probes such as DCFH-DA. Apoptosis is assessed by Annexin V/PI staining and caspase activity assays. The compound demonstrates concentration-dependent induction of ROS and apoptosis. |
| Animal Protocol |
In vivo animal studies for 6-Formylpterin are limited, as the compound is primarily studied in vitro. For efficacy testing, animal models of disease could be used. Animals would be treated with 6-Formylpterin via oral or intraperitoneal administration at various doses, and relevant biomarkers would be assessed. However, detailed in vivo protocols are not well established in the available literature.
|
| ADME/Pharmacokinetics |
6-Formylpterin has a molecular formula of C7H5N5O2 and a molecular weight of 191.15. It appears as a solid with a purity of ≥95%. It is soluble in water at 33.33 mg/mL (174.37 mM) with pH adjustment to 12 with 1 M NaOH. The compound is sparingly soluble in DMSO. It should be stored at -20°C, protected from light, and stored under nitrogen. In solvent, it is stable at -80°C for 6 months and at -20°C for 1 month (protected from light, stored under nitrogen). It is intended for research use only and is not for human consumption.
|
| Toxicity/Toxicokinetics |
The toxicity profile of 6-Formylpterin has not been extensively characterized. As a folate metabolite and xanthine oxidase inhibitor, it is generally considered to have low toxicity. Standard toxicity studies would include assessment of acute oral toxicity, repeated-dose toxicity, and genotoxicity in animal models. The compound is intended for research use only and is not approved for clinical use.
|
| References | |
| Additional Infomation |
6-Formylpterin is a pterin with a formyl group at the 6-position. It is an inhibitor of xanthine oxidase (EC 1.17.3.2) and a reactive oxygen species generator. It belongs to the pterin class of compounds and is also an aldehyde compound.
6-Formylpterin (CAS 712-30-1) is a xanthine oxidase inhibitor that induces ROS generation and apoptosis. It has a molecular formula of C7H5N5O2 and a molecular weight of 191.15. It is a Vitamin B9 (folate) metabolite and a ligand to MR1 antigens presented on MAIT cells. The compound inhibits xanthine oxidase and induces apoptosis in HL-60 cells. It is intended for research use only and is not approved for clinical use. |
| Molecular Formula |
C7H5N5O2
|
|---|---|
| Molecular Weight |
191.15
|
| Exact Mass |
191.044
|
| CAS # |
712-30-1
|
| PubChem CID |
135409352
|
| Appearance |
Light yellow to brown solid powder
|
| Density |
1.9±0.1 g/cm3
|
| Boiling Point |
489.1ºC at 760 mmHg
|
| Flash Point |
249.6ºC
|
| Index of Refraction |
1.893
|
| LogP |
-1.77
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
14
|
| Complexity |
303
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LLJAQDVNMGLRBD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C7H5N5O2/c8-7-11-5-4(6(14)12-7)10-3(2-13)1-9-5/h1-2H,(H3,8,9,11,12,14)
|
| Chemical Name |
2-amino-4-oxo-3H-pteridine-6-carbaldehyde
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 5.2315 mL | 26.1575 mL | 52.3149 mL | |
| 5 mM | 1.0463 mL | 5.2315 mL | 10.4630 mL | |
| 10 mM | 0.5231 mL | 2.6157 mL | 5.2315 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.