| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Minoxidil-d10 is a stable isotope-labeled internal standard and not primarily a pharmacologically active compound. The non-deuterated parent compound minoxidil targets ATP-sensitive potassium channels (KATP) in vascular smooth muscle and hair follicles. By opening KATP channels, minoxidil causes hyperpolarization of smooth muscle cells, leading to vasodilation and reduced peripheral vascular resistance. Minoxidil also activates cyclooxygenase-1 (COX-1) (AC50 = 80 uM), increasing prostaglandin E2 (PGE2) production, which contributes to hair growth stimulation.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Minoxidil (non-deuterated) activates cyclooxygenase-1 (COX-1) with an AC50 of 80 uM in BALB/c 3T3 fibroblasts and human dermal papilla fibroblasts, increasing prostaglandin E2 production. It is a potent vasodilator that opens ATP-sensitive potassium channels (KATP) in arteriolar smooth muscle. Minoxidil-d3 (not d10) has been used in LC-MS studies to measure minoxidil concentrations. Minoxidil is known to activate the Kir6.1/SUR2B channel (vascular KATP) and shows specificity for vascular over pancreatic KATP channels. |
| ln Vivo |
Minoxidil (non-deuterated) is an effective oral antihypertensive agent that reduces blood pressure by opening ATP-sensitive potassium channels in vascular smooth muscle, leading to peripheral vasodilation. Topical minoxidil is used to treat androgenetic alopecia (male and female pattern hair loss). Minoxidil-d10 is used as an internal standard for quantification and is not administered for efficacy studies. For pharmacokinetic studies, minoxidil-d10 is spiked into biological samples to track minoxidil levels.
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| Enzyme Assay |
The primary use of minoxidil-d10 is as an internal standard for LC-MS or GC-MS quantification. For assay development, calibration standards are prepared by spiking known amounts of non-deuterated minoxidil into blank plasma or other biological matrices, along with a fixed amount of minoxidil-d10 (e.g., 50 ng/mL). Standard curves are generated by plotting the peak area ratio (minoxidil/minoxidil-d10) against minoxidil concentration. For receptor binding studies, membranes from cells expressing KATP channels (e.g., Kir6.2/SUR1 or Kir6.1/SUR2B) are incubated with [3H]P1075 or [3H]minoxidil sulfate in the presence of unlabeled compounds.
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| Cell Assay |
Minoxidil-d10 is not typically used in cell-based assays as a test article because it is an internal standard. For studies of the non-deuterated parent compound, dermal papilla cells (DPCs) or fibroblasts are treated with minoxidil (0.1-100 uM) for 24-72 hours. Prostaglandin E2 (PGE2) levels are measured by ELISA. Cyclooxygenase-1 (COX-1) activity is assessed by measuring PGE2 production in the presence of arachidonic acid. KATP channel activity can be assessed by measuring membrane potential using voltage-sensitive dyes (e.g., DiBAC4(3)) or by rubidium (86Rb) efflux assays. For viability studies, MTT or Alamar Blue assays are performed.
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| Animal Protocol |
Minoxidil-d10 is not typically used in vivo as a test article; it is an internal standard. For pharmacokinetic studies using minoxidil-d10 as an internal standard, the compound is administered as a tracer or spiked into collected samples. Non-deuterated minoxidil is formulated in water or saline for oral administration (0.5-5 mg/kg) to rats or dogs for PK studies. Topical minoxidil (2% or 5% solution) is applied to shaved skin on the backs of mice or rats for hair growth studies. Blood samples are collected at various time points, and minoxidil levels are quantified by LC-MS using minoxidil-d10 as the internal standard.
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| ADME/Pharmacokinetics |
Minoxidil-d10 is used as an internal standard in LC-MS or GC-MS assays. For minoxidil pharmacokinetic studies, the non-deuterated compound is administered orally (in dogs or rats) or topically (in minoxidil solution). In humans, oral minoxidil has a bioavailability of approximately 90-100%, a half-life of 4-5 hours, and is metabolized primarily by glucuronidation. Topical minoxidil has low systemic absorption (approximately 1-2%). Minoxidil-d10 elutes at a slightly different retention time but co-elutes with minoxidil under most conditions, allowing accurate quantification. The compound is stable in plasma for at least 24 hours at room temperature.
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| Toxicity/Toxicokinetics |
Minoxidil-d10 is not toxic at the concentrations used for internal standards (typically ng/mL to ug/mL range). The non-deuterated parent compound minoxidil has known side effects including hypertrichosis (excessive hair growth), fluid retention, tachycardia, and pericardial effusion at high oral doses. Topical minoxidil is generally well tolerated, with mild skin irritation in some users. Systemic toxicity is rare with topical use. Minoxidil-d10 is not expected to have significant toxicity when used as an internal standard in analytical assays. Standard laboratory safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
Minoxidil-d10 is a research tool for analytical chemistry and pharmacokinetic studies. It is not approved for therapeutic use. The compound is used to accurately quantify minoxidil levels in biological samples by mass spectrometry, supporting studies of minoxidil pharmacokinetics, drug metabolism, and topical absorption. The presence of 10 deuterium atoms on the piperidine ring provides a mass shift of +10 Da relative to non-deuterated minoxidil, allowing clear differentiation by mass spectrometry. The compound is stored at -20degC as a solid, protected from light and moisture.
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| Molecular Formula |
C9H5D10N5O
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|---|---|
| Molecular Weight |
219.31
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| Exact Mass |
219.19
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| CAS # |
1020718-66-4
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| PubChem CID |
45039940
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
544.9±60.0 °C at 760 mmHg
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| Flash Point |
283.4±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.724
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| LogP |
-0.41
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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 |
[2H]C1(C(C(N(C(C1([2H])[2H])([2H])[2H])C2=NC(=N)N(C(=C2)N)O)([2H])[2H])([2H])[2H])[2H]
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| InChi Key |
ZIMGGGWCDYVHOY-YXALHFAPSA-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/i1D2,2D2,3D2,4D2,5D2
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| Chemical Name |
6-(2,2,3,3,4,4,5,5,6,6-decadeuteriopiperidin-1-yl)-3-hydroxy-2-iminopyrimidin-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) |
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
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| 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 | 4.5598 mL | 22.7988 mL | 45.5976 mL | |
| 5 mM | 0.9120 mL | 4.5598 mL | 9.1195 mL | |
| 10 mM | 0.4560 mL | 2.2799 mL | 4.5598 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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