Tetrahydrobiopterin
Based on 3 publication(s) in Google Scholar
Tetrahydrobiopterin ((Rac)-Sapropterin) is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
For research use only. We do not sell to patients.
- Purity: 98.95%
- CAS No.: 17528-72-2
- Formula: C9H15N5O3
- Molecular Weight:241.25
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Tetrahydrobiopterin
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In Vivo Efficacy Study
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Histological Imaging/Staining
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IF
All Endogenous Metabolite Isoforms
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Biological Activity
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Human Endogenous Metabolite |
MicMicroglial cell cultures under hyperoxia are supplemented or not with an effective dose of Tetrahydrobiopterin (BH4) (100 μM). Exposure of microglial cells to hyperoxia-induced oxidative stress for 24 h reveals a robust increase in TSP-1 mRNA expression and protein compare to normoxia (21% O2). Tetrahydrobiopterin supplementation significantly prevents hyperoxia-induced microglial activation by diminishing Iba-1 and TSP-1 expression? and prevents microvascular injury in choroidal explants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 17528-72-2
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Appearance Solid
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Molecular Weight 241.25
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Formula C9H15N5O3
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Color White to off-white
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SMILES
O=C1C2=C(NC(N)=N1)NCC(C(O)C(O)C)N2
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Synonyms
(Rac)-Sapropterin
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
S100A4 regulates ferroptosis to suppress cell proliferation via the SLC7A11-GSH axis but facilitates Brucella infection in RAW264.7 macrophages. [Abstract]2025 Dec;333(Pt 1):148831. PMID: 41203174 -
Free Radic Biol Med
Intermedin protects peritubular capillaries by inhibiting eNOS uncoupling through AMPK/GTPCH-I/BH4 pathway and alleviate CKD following AKI. [Abstract]2025 Apr 12:S0891-5849(25)00225-4. PMID: 40228707
Tetrahydrobiopterin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Apr 12:S0891-5849(25)00225-4. [Abstract]
Tetrahydrobiopterin (BH4, 100 μM; 24 h). The levels of eNOS monomer and dimer in different groups were detected using western blotting.
Tetrahydrobiopterin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Apr 12:S0891-5849(25)00225-4. [Abstract]
Tetrahydrobiopterin (BH4, 100 μM; 24 h). Representative immunofluorescence staining of ROS (red) with nuclear stain (DAPI, blue) in HUVECs (scale bar, 50 μm; n = 6).
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CNS Neurosci Ther
Ferroptosis-Driven Neuronal Damage Exacerbation in Diabetic Stroke: Implications of SLC7A11 Inhibition. [Abstract]2026 Mar;32(3):e70830. PMID: 41820788
Tetrahydrobiopterin purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2026 Mar;32(3):e70830. [Abstract]
Tetrahydrobiopterin (BH4, 10 mg/kg; once daily for five days). Representative TTC-stained brain sections of db/db mice treated with vehicle or ferroptosis inhibitors at 24 h post-reperfusion.
Tetrahydrobiopterin purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2026 Mar;32(3):e70830. [Abstract]
Tetrahydrobiopterin (BH4, 10 mg/kg; once daily for five days). Representative images and quantification of HE staining and NeuN staining at 24 h post-reperfusion in the ischemic penumbra. Red arrows denote pyknotic nuclei (n = 5/group). Scale bars = 10 μm.
Solvent & Solubility
DMSO : 50 mg/mL (207.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Microglia cell line (SIM-A9) is used and cultured. Briefly, microglial cells (800, 000 cells per well) are cultured in 6-well plates with DMEM/F12 (1:1) supplementing with 10% fetal bovine serum (FBS), 5% of horse serum (HS), and 1% penicillin/streptomycin. After 24 h, the cells are starved with DMEM/F12 (1:1) free of FBS and HS for 6 h. Then, microglial cells cultures in presence or absence of 100 μM of Tetrahydrobiopterin are exposed to hyperoxia (75% oxygen and 25% nitrogen) in a modular incubator chamber and maintained in a humidified CO2 incubator at 37 °C for 24 h. Microglial cells in matching controls are incubated at 37 °C in an incubator with 95% air and 5% CO2 and collected at the same time point. Cell lysates are quickly processed for RNA. The conditioning media is stored at -80 and later used in choroidal explant assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice pups are exposed with their mothers in a 75% oxygen environment from postnatal day 7 to P9 using oxycycler to induce retinal vaso-obliteration (VO). Animals are anesthetized and injected intravitreally at P7 with 100 μM of Tetrahydrobiopterin or vehicle (sterile PBS 1×) using a syringe equipped with 50-gauge glass capillary. At P9, mice pups are sacrificed and retinas are dissected and stained overnight at 4 °C with fluorescein-labeled Griffonia Simplicifolia Lectin 1 (GSL 1), isolectin B4 (1:100) with 1 mM CaCl2 in PBS. Quantification of VO is assessed using the computer software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.1451 mL | 20.7254 mL | 41.4508 mL | 103.6269 mL |
| 5 mM | 0.8290 mL | 4.1451 mL | 8.2902 mL | 20.7254 mL | |
| 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 mL | 10.3627 mL | |
| 15 mM | 0.2763 mL | 1.3817 mL | 2.7634 mL | 6.9085 mL | |
| 20 mM | 0.2073 mL | 1.0363 mL | 2.0725 mL | 5.1813 mL | |
| 25 mM | 0.1658 mL | 0.8290 mL | 1.6580 mL | 4.1451 mL | |
| 30 mM | 0.1382 mL | 0.6908 mL | 1.3817 mL | 3.4542 mL | |
| 40 mM | 0.1036 mL | 0.5181 mL | 1.0363 mL | 2.5907 mL | |
| 50 mM | 0.0829 mL | 0.4145 mL | 0.8290 mL | 2.0725 mL | |
| 60 mM | 0.0691 mL | 0.3454 mL | 0.6908 mL | 1.7271 mL | |
| 80 mM | 0.0518 mL | 0.2591 mL | 0.5181 mL | 1.2953 mL | |
| 100 mM | 0.0415 mL | 0.2073 mL | 0.4145 mL | 1.0363 mL |
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