| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
7,8-Dihydroneopterin does not have a classical drug target but is involved in multiple biological processes. It acts as a cofactor for certain enzymes and as a precursor for BH4, which is an essential cofactor for aromatic amino acid hydroxylases (e.g., phenylalanine hydroxylase, tyrosine hydroxylase, tryptophan hydroxylase) and nitric oxide synthases (NOS). Additionally, it serves as a potent antioxidant and immune modulator.
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| ln Vitro |
7,8-Dihydroneopterin is a heterocyclic pteridine that is generated and secreted by macrophages and monocytes in response to the cytokine interferon-y (IFN-y) [1]. Inhibiting the proliferation of U373MG astrocytes, 7,8-DiHydroneopterin (0.1, 0.5, 1, 2.5, 5 mM; 2 days and 5 days) [1].
In vitro, 7,8-dihydroneopterin exhibits concentration-dependent antioxidant activity, scavenging reactive oxygen species (ROS) including superoxide (O2-) and peroxynitrite (ONOO-). It also modulates immune responses by inducing the expression of pro-inflammatory cytokines such as IL-1beta, IL-6, and TNF-alpha in activated macrophages. The compound has been shown to inhibit tetrahydrobiopterin (BH4)-dependent enzyme activities by competing for binding sites. |
| ln Vivo |
For antioxidant assays, 7,8-dihydroneopterin (0.1-100 uM) is incubated with a superoxide-generating system (e.g., xanthine/xanthine oxidase) and the superoxide-sensitive probe dihydroethidium (DHE) or cytochrome c in PBS at 37degC for 15-30 min. Superoxide scavenging activity is measured by fluorescence or absorbance reduction and compared to reference standards such as Trolox or ascorbic acid.
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| Enzyme Assay |
A typical biochemical assay for dihydroneopterin is its conversion to biopterin under oxidative conditions. However, receptor-binding assays are not applicable as this compound is not a direct enzyme/receptor agonist/antagonist. For cellular assays, primary mouse peritoneal macrophages or RAW 264.7 cells are seeded in 96-well plates and treated with 7,8-dihydroneopterin (1-100 uM) for 6-24 h. Cell supernatants are collected for cytokine measurement by ELISA (IL-1beta, IL-6, TNF-alpha). Alternatively, cells are stimulated with LPS (100 ng/mL) concurrently with 7,8-dihydroneopterin, and NF-kappaB activation is measured by Western blot. For ROS measurement, cells are loaded with DCFH-DA (10 uM) for 30 min before treatment, and fluorescence is monitored.
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Astrocyte line U373MG Tested Concentrations: 0.1, 0.5, 1, 2.5, 5 mM Incubation Duration: 2 days and 5 days Experimental Results: After 2 days of treatment, a significant decrease in the number of cells in these cells was observed. 5 mM and 2.5 mM treated cells. After 5 days of incubation, concentrations of 1-5 mM completely eliminated acid phosphatase activity to background levels in complete cell culture medium. Significant cell growth inhibition was also seen for cells incubated with 0.5 mM, whereas 0.1 mM did not alter cell growth. |
| Animal Protocol |
In vivo studies with 7,8-dihydroneopterin are limited. It can be administered to mice via intraperitoneal injection at 1-20 mg/kg in PBS to evaluate its immunomodulatory effects. In rodent models of inflammation (e.g., LPS-induced sepsis or carrageenan-induced paw edema), plasma and tissue levels of 7,8-dihydroneopterin are measured as a biomarker of oxidative stress. The neopterin-to-dihydroneopterin ratio is used to assess the severity of immune activation.
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| ADME/Pharmacokinetics |
7,8-Dihydroneopterin is an endogenous metabolite; its PK properties are not typically studied as a drug candidate. In humans, baseline plasma levels are generally low (nM range) but increase significantly during immune activation (e.g., viral infections, autoimmune diseases). The compound is rapidly oxidized to neopterin or converted to BH4 in tissues. Renal excretion is the primary elimination route, with neopterin serving as a stable urinary biomarker.
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| Toxicity/Toxicokinetics |
As an endogenous compound, 7,8-dihydroneopterin is generally considered non-toxic at physiological levels. Elevated levels are observed in inflammatory conditions but are thought to reflect immune activation rather than cause toxicity. No specific toxicity data are available for exogenous administration. Safety assessments are not applicable as this compound is not a drug candidate but rather a research tool and biomarker.
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| References | |
| Additional Infomation |
7,8-Dihydroneopterin is a pterin with hydrogenated C-7 and C-8 positions. It is a metabolite found in humans, Saccharomyces cerevisiae, Escherichia coli, and mice. It is a dihydropterin belonging to the neopterin family. 7,8-Dihydroneopterin is a metabolite found or produced in Escherichia coli (K12 strain, MG1655 strain). 7,8-Dihydroneopterin has also been reported in humans and methanococci, with relevant data available. 7,8-Dihydroneopterin is a metabolite found or produced in Saccharomyces cerevisiae.
7,8-Dihydroneopterin is an intermediate in tetrahydrobiopterin (BH4) biosynthesis and a biomarker of oxidative stress and immune activation. Elevated levels are associated with inflammatory diseases, viral infections, and certain cancers. The neopterin/dihydroneopterin ratio is a clinical biomarker for monitoring disease progression and response to therapy. The compound is not a drug and has no therapeutic approval status. |
| Molecular Formula |
C₉H₁₃N₅O₄
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|---|---|
| Molecular Weight |
255.23
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| Exact Mass |
255.097
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| CAS # |
1218-98-0
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| PubChem CID |
135398602
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| Appearance |
Light yellow to yellow solid powder
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| Density |
2.03g/cm3
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| Boiling Point |
614.6ºC at 760mmHg
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| Flash Point |
325.5ºC
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| Vapour Pressure |
1.13E-17mmHg at 25°C
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| Index of Refraction |
1.86
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| LogP |
-3.3
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
470
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C(=NC2=C(N1)N=C(NC2=O)N)[C@@H]([C@@H](CO)O)O
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| InChi Key |
YQIFAMYNGGOTFB-XINAWCOVSA-N
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| InChi Code |
InChI=1S/C9H13N5O4/c10-9-13-7-5(8(18)14-9)12-3(1-11-7)6(17)4(16)2-15/h4,6,15-17H,1-2H2,(H4,10,11,13,14,18)/t4-,6+/m1/s1
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| Chemical Name |
2-amino-6-[(1S,2R)-1,2,3-trihydroxypropyl]-7,8-dihydro-3H-pteridin-4-one
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| Synonyms |
7,8Dihydroneopterin; 7,8 Dihydroneopterin
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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 : ~250 mg/mL (~979.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (24.49 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 62.5 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: ≥ 2.08 mg/mL (8.15 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 20.8 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: ≥ 2.08 mg/mL (8.15 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 | 3.9180 mL | 19.5902 mL | 39.1803 mL | |
| 5 mM | 0.7836 mL | 3.9180 mL | 7.8361 mL | |
| 10 mM | 0.3918 mL | 1.9590 mL | 3.9180 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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