| Size | Price | Stock | Qty |
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| 5g |
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| Targets |
Endogenous Metabolite
Minoxidil acts as an ATP-sensitive potassium channel opener on vascular smooth muscle cells. By opening these channels, it hyperpolarizes the cell membrane, leading to relaxation of smooth muscle and vasodilation. This reduces peripheral vascular resistance and lowers blood pressure. For hair growth, minoxidil is believed to stimulate hair follicles by increasing blood flow and by prolonging the anagen (growth) phase of the hair cycle. |
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| ln Vitro |
Using minoxidil (1-00 μM; 24 h; RAMEC cells) demonstrated extremely minimal cytotoxicity over the whole concentration range (from 1 μM to 100 μM) that was investigated [1].
In vitro, minoxidil has been shown to stimulate the proliferation of human hair follicle dermal papilla cells. It also increases the expression of vascular endothelial growth factor (VEGF) and other growth factors in these cells, which may promote hair growth. In vascular smooth muscle cells, it causes relaxation and vasodilation, which is the basis for its antihypertensive effect. |
| ln Vivo |
Rats treated with minoxidil (0.01 mmol/kg body weight; intraperitoneal injection; 3.5 hours duration; Fisher 344 rats) showed 49% inhibitory efficacy in preventing carrageenan-induced paw edema [1].
In vivo, oral minoxidil is a potent vasodilator that effectively lowers blood pressure in patients with severe hypertension. Topical minoxidil is applied to the scalp and is used to treat male and female pattern baldness. It has been shown to increase hair regrowth and slow the progression of hair loss in a significant proportion of users. The mechanism of action for hair growth is not fully understood. |
| Enzyme Assay |
The in vitro receptor/enzyme binding assay for minoxidil involves measuring its ability to open ATP-sensitive potassium channels. This is typically done using electrophysiological techniques (patch-clamp) on cells expressing these channels. The increase in potassium current upon application of minoxidil is measured to determine its potency as a channel opener.
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| Cell Assay |
In vitro cellular assays for minoxidil are performed on hair follicle dermal papilla cells. Cells are treated with minoxidil, and parameters related to cell proliferation (e.g., DNA synthesis) and growth factor expression (e.g., VEGF, FGF-7) are measured. The ability of minoxidil to stimulate cell growth and to increase the expression of pro-hair growth factors is assessed.
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| Animal Protocol |
Animal/Disease Models: Fisher 344 rat (150-200 g) edema [1]
Doses: 0.01 mmol/kg body weight Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. 3.5 hrs (hrs (hours)) Experimental Results: Inhibits carrageenan-induced edema. In vivo animal experiments for minoxidil have been conducted in various models. For antihypertensive studies, spontaneously hypertensive rats (SHR) are used to measure the reduction in blood pressure after oral administration. For hair growth studies, animal models such as the C3H/HeJ mouse, which undergoes cyclic hair loss, or the stumptailed macaque, which develops baldness, are used to evaluate the efficacy of topical minoxidil. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known human metabolites of minoxidil include 2-pyrimidinamine and 1,6-dihydro-6-imino-4-(1-piperidinyl)-1-(sulfonoxy)-. Oral minoxidil is rapidly and completely absorbed from the gastrointestinal tract. It is primarily metabolized in the liver to its active metabolite, minoxidil sulfate, which is responsible for its vasodilatory activity. The drug is excreted primarily in the urine. Its half-life is approximately 4.2 hours. Topical minoxidil is minimally absorbed systemically; only about 1.4% of an applied dose is absorbed through the scalp. |
| Toxicity/Toxicokinetics |
Oral minoxidil can cause significant side effects due to its potent vasodilatory effect. Common side effects include tachycardia, fluid retention (edema), and hypertrichosis (excessive hair growth). Topical minoxidil is generally well-tolerated but can cause local irritation, itching, and dryness at the application site. Allergic reactions are rare. It is not recommended for use in patients with pheochromocytoma or those with a history of myocardial infarction.
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| References |
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| Additional Infomation |
Minoxidil is a pyrimidine N-oxide, namely pyrimidine-2,4-diamine-3-oxide, with a piperidine-1-yl substitution at the 6-position. It has vasodilatory and antihypertensive effects. It is a pyrimidine N-oxide belonging to the piperidine and aminopyrimidine classes of compounds. Minoxidil is a small artery vasodilator. Its physiological action is achieved by dilating small arteries. It is a potent, direct-acting vasodilator (vasodilator) that reduces peripheral resistance and lowers blood pressure. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 371) See also: Minoxidil (note moved to).
Minoxidil is marketed under the brand name Rogaine for topical use and Loniten for oral use. It was approved by the FDA as a topical treatment for hair loss in 1988 and as an oral antihypertensive in 1979. It is one of the few FDA-approved treatments for androgenetic alopecia. Its exact mechanism for hair growth remains an area of active research, but it is considered the first-line treatment for this condition alongside finasteride. |
| Molecular Formula |
C9H15N5O
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|---|---|
| Molecular Weight |
209.2483
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| Exact Mass |
209.127
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| Elemental Analysis |
C, 51.66; H, 7.23; N, 33.47; O, 7.65
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| CAS # |
38304-91-5
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| Related CAS # |
38304-91-5; 69935-18-8; 83701-22-8; 1020718-66-4
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| PubChem CID |
4201
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| Appearance |
White to off-white solid
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
351.7±45.0 °C at 760 mmHg
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| Melting Point |
272-274 °C (dec.)(lit.)
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| Flash Point |
166.5±28.7 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.724
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| Source |
Endogenous Metabolite
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| LogP |
-1.49
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
329
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])N1/C(=N/[H])/N=C(C([H])=C1N([H])[H])N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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| InChi Key |
ZIMGGGWCDYVHOY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H15N5O/c10-7-6-8(12-9(11)14(7)15)13-4-2-1-3-5-13/h6,11,15H,1-5,10H2
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| Chemical Name |
3-hydroxy-2-imino-6-piperidin-1-ylpyrimidin-4-amine
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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) |
Ethanol : ~7.14 mg/mL (~34.12 mM)
H2O : ~1 mg/mL (~4.78 mM ) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (3.39 mM) (saturation unknown) in 10% EtOH + 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 7.1 mg/mL clear EtOH 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: ≥ 0.71 mg/mL (3.39 mM) (saturation unknown) in 10% EtOH + 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 7.1 mg/mL clear EtOH 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: ≥ 0.71 mg/mL (3.39 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.5 mg/mL (2.39 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 5.0 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 5: ≥ 0.5 mg/mL (2.39 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 5.0 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. Solubility in Formulation 6: ≥ 0.5 mg/mL (2.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: 1.96 mg/mL (9.37 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Solubility in Formulation 8: 5 mg/mL (23.89 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7790 mL | 23.8949 mL | 47.7897 mL | |
| 5 mM | 0.9558 mL | 4.7790 mL | 9.5579 mL | |
| 10 mM | 0.4779 mL | 2.3895 mL | 4.7790 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.
Topical or Oral Minoxidil for the Treatment of Endocrine Therapy-Induced Alopecia in Patients With Stage I-IV Breast Cancer
CTID: NCT05417308
PhaseEarly Phase 1 Status: Recruiting
Date: 2024-05-31
Products are for research use only; We do not sell to patients
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