| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
IC50: K channel[2]
The primary target of minoxidil sulfate is the ATP-sensitive potassium (KATP) channel, specifically the Kir6.x/SUR2B subtype found in vascular smooth muscle cells. By binding to and opening these channels, minoxidil sulfate causes membrane hyperpolarization, which reduces calcium influx through voltage-gated calcium channels. This leads to relaxation of vascular smooth muscle and vasodilation. In the context of hair growth, the opening of KATP channels in dermal papilla cells is believed to stimulate hair follicle proliferation and prolong the anagen (growth) phase. Minoxidil sulfate is the active metabolite responsible for the pharmacological effects of its parent compound, minoxidil. |
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| ln Vitro |
Blood-brain tumor barrier (BTB) permeability in RBMEC monolayers is significantly reduced by minoxidil suLfate (1-100 μM; 2 hours) in a time-dependent manner. Additionally, high concentrations of MS have a high effect on transendothelial electrical resistance (TEER) after 2 hours[2]. In brain tumor tissue, minoxidil sulfate (0-100 μM; 0-4 hours) elevated RhoA activity for 1 hour, peaking at 2 hours. Moreover, it strongly increased PKB phosphorylation at Ser-473 in a transitory manner without changing PKB levels overall. Furthermore, LY294002 partially inhibits PKB phosphorylation produced by MS [2].
In vitro, minoxidil sulfate is a potent relaxant of vascular smooth muscle with an IC50 of 0.14 µM. It acts as a selective ATP-sensitive potassium channel opener, and its activity is often studied in isolated vascular ring preparations or cultured smooth muscle cells. In cell-based assays, minoxidil sulfate has been shown to stimulate the proliferation of dermal papilla cells and prolong their survival, which is believed to underlie its hair growth-promoting effects. The compound is soluble in DMSO at 25 mg/ml and is used to study KATP channel pharmacology and its role in vasodilation and hair growth. |
| ln Vivo |
In vivo, minoxidil sulfate is the pharmacologically active metabolite responsible for the vasodilatory and hair growth-promoting effects observed with minoxidil administration. In animal models, it promotes hair growth, likely through the stimulation of dermal papilla cells and the prolongation of the anagen phase. Its vasodilatory action contributes to its antihypertensive effects, as it reduces peripheral vascular resistance by relaxing arterial smooth muscle. The compound's ability to open KATP channels in various tissues underlies its diverse pharmacological actions, including its effects on blood pressure and hair follicle biology.
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| Enzyme Assay |
In vitro assays for studying minoxidil sulfate typically involve functional measurements of KATP channel activity using patch-clamp electrophysiology on isolated smooth muscle cells or cell lines expressing recombinant KATP channels. Vasorelaxation assays are performed using isolated arterial rings from animal models, where the compound's ability to relax pre-contracted vessels is measured in a tissue bath. The concentration-response relationship is determined to calculate the EC50 or IC50 for vasorelaxation. Additionally, binding studies using radiolabeled ligands such as [3H]glibenclamide can be used to assess the compound's interaction with the sulfonylurea receptor (SUR) subunit of the KATP channel.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: Rat brain microvascular endothelial cells (RBMECs) Tested Concentrations: 0-100 μM Incubation Duration: 15 mins, 30 mins, 1 hour, 2 hrs (hours), 4 hrs (hours) Experimental Results: Induced RhoA activation and PKB phosphorylation at Ser -473. Cellular assays for minoxidil sulfate often utilize dermal papilla cells (DPCs) to study its effects on hair growth. DPCs are cultured and treated with varying concentrations of minoxidil sulfate (typically in the micromolar range), and cell proliferation is measured using assays such as MTT or BrdU incorporation. The compound's effects on cell survival, apoptosis, and the expression of growth factors (e.g., VEGF, HGF) are also assessed. In vascular smooth muscle cells, the compound's ability to increase potassium efflux and hyperpolarize the cell membrane can be measured using fluorescent membrane potential dyes or patch-clamp electrophysiology. |
| Animal Protocol |
In vivo animal studies for minoxidil sulfate are often conducted in rodent models to evaluate its hair growth-promoting effects. The compound can be administered topically (as a solution applied to shaved skin) or systemically (via oral gavage or subcutaneous injection). Endpoints include hair regrowth assessment (by measuring the area or weight of hair regrowth), histological analysis of hair follicles (to determine the number and size of follicles and the duration of the anagen phase), and immunohistochemical staining for proliferation markers (such as Ki67) or growth factors. For cardiovascular studies, blood pressure measurements and vascular reactivity tests are performed to assess the vasodilatory effects of the compound.
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| ADME/Pharmacokinetics |
Minoxidil sulfate is the active metabolite of minoxidil, and its pharmacokinetic properties are often discussed in the context of the parent drug. Following topical application of minoxidil, it is absorbed through the skin and metabolized by sulfotransferase enzymes in the hair follicle and skin to form minoxidil sulfate. The compound is then distributed to the target tissues, where it exerts its effects. Systemic absorption of topically applied minoxidil is limited, and the compound is primarily excreted in the urine. The pharmacokinetic profile of minoxidil sulfate is characterized by its rapid formation and local action at the site of application.
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| Toxicity/Toxicokinetics |
There is no specific toxicity data reported for minoxidil sulfate in the available literature beyond its classification as a research chemical. However, as the active metabolite of minoxidil, its safety profile is considered in the context of the parent drug. Minoxidil sulfate is not approved for human use as a standalone therapeutic agent. As a research chemical, it should be handled with standard safety precautions for laboratory use, including the use of appropriate personal protective equipment. Researchers should consult the material safety data sheet (MSDS) for detailed safety and handling information.
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| References |
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| Additional Infomation |
Minoxidil metabolites; structures are described in the first reference.
Minoxidil sulfate (U-58838) is a potent and selective ATP-sensitive K+ channel opener and the active metabolite of minoxidil. It is a potent vascular smooth muscle relaxant with an IC50 of 0.14 µM. The compound is considered a vasodilator and promotes hair growth in experimental animal models. Minoxidil sulfate is supplied with a purity of ≥98% and is used in research to study KATP channel pharmacology, vasodilation, and hair growth mechanisms. It is soluble in DMSO at 25 mg/ml. |
| Molecular Formula |
C9H15N5O4S
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|---|---|
| Molecular Weight |
289.31
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| Exact Mass |
289.084
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| CAS # |
83701-22-8
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| Related CAS # |
38304-91-5; 69935-18-8; 83701-22-8; 1020718-66-4
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| PubChem CID |
138113345
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| Appearance |
White to off-white solid powder
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| Boiling Point |
732ºC at 760 mmHg
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| Melting Point |
175-180°C
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| Flash Point |
396.5ºC
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| LogP |
0.72
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
529
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(CC1)C2=CC(=N)N(C(=N2)N)OS(=O)(=O)O
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| InChi Key |
KVOZMWUBYWDGEX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H15N5O4S/c10-7-6-8(13-4-2-1-3-5-13)12-9(11)14(7)18-19(15,16)17/h6,10H,1-5H2,(H2,11,12)(H,15,16,17)
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| Chemical Name |
(2-amino-6-imino-4-piperidin-1-ylpyrimidin-1-yl) hydrogen sulfate
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| Synonyms |
U-10858; U10858 sulfate
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (864.12 mM)
H2O: 50 mg/mL (172.82 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.19 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 20.8 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 (7.19 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 (7.19 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 | 3.4565 mL | 17.2825 mL | 34.5650 mL | |
| 5 mM | 0.6913 mL | 3.4565 mL | 6.9130 mL | |
| 10 mM | 0.3457 mL | 1.7282 mL | 3.4565 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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