| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
4-Hydroxy xylazine is the hydroxylated metabolite of xylazine, which is an agonist of α2-adrenergic receptors. As a metabolite, it may retain some α2-adrenergic receptor binding activity. Xylazine is used for sedation, anesthesia, and analgesia in non-human mammals. 4-Hydroxy xylazine serves as a marker for xylazine doping in equine urine and is used for analytical forensic applications.
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| ln Vitro |
In vitro activity of 4-Hydroxy xylazine is related to its role as a xylazine metabolite. It may retain some α2-adrenergic receptor binding activity. The compound is used as an analytical reference standard for detecting xylazine doping in horses. Detailed in vitro activity data, including receptor binding affinity, are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity of 4-Hydroxy xylazine is related to its role as a metabolite of xylazine. It is found in urine as a minor urinary metabolite in most patients. The compound is used as a marker for xylazine exposure and doping. Detailed in vivo pharmacokinetic and pharmacodynamic data are not extensively documented in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for 4-Hydroxy xylazine typically involves measuring its binding affinity to α2-adrenergic receptors. Competitive binding assays using radiolabeled ligands and membrane preparations from tissues expressing α2-adrenergic receptors are performed. The compound's ability to displace the radioligand is measured, and binding affinity is determined. Standard protocols include xylazine as a positive control.
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| Cell Assay |
In vitro cell-based assays for 4-Hydroxy xylazine are not typically applicable, as the compound is primarily used as an analytical reference standard and metabolite marker. However, cell-based assays measuring α2-adrenergic receptor activation may be performed to assess its pharmacological activity. Standard protocols include xylazine as a positive control and appropriate vehicle controls.
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| Animal Protocol |
In vivo animal studies for 4-Hydroxy xylazine are typically conducted for analytical and toxicological evaluation. Animals administered xylazine have 4-hydroxy xylazine detected in urine as a metabolite. The compound is used as a marker for xylazine doping in horses. Toxicological studies may evaluate its presence in polydrug detection. Detailed in vivo protocols are not extensively documented.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 4-Hydroxy xylazine include a molecular weight of 236.33 and a molecular formula of C12H16N2OS. As a metabolite of xylazine, it is found in urine. Purity is reported as ≥97%. Storage recommendations include conditions specified in the Certificate of Analysis. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Toxicity information for 4-Hydroxy xylazine is related to its role as a metabolite of xylazine. Xylazine is an α2-adrenergic agonist used in veterinary medicine. The toxicity of the metabolite may be evaluated in the context of xylazine exposure. Standard safety precautions for handling research chemicals should be followed. No detailed toxicity data are available.
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| References |
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| Additional Infomation |
4-Hydroxy xylazine (Xylazine Impurity 10, Compound M2) is the primary hydroxylated metabolite of xylazine, an α2-adrenergic agonist used in veterinary medicine. It is used as a marker for xylazine doping in horses and for analytical forensic applications. It has MW 236.33 and formula C12H16N2OS. It is intended for research use only.
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| Molecular Formula |
C12H16N2OS
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|---|---|
| Molecular Weight |
236.33
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| Exact Mass |
236.098
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| CAS # |
145356-32-7
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| PubChem CID |
46781929
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
391.7±52.0 °C at 760 mmHg
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| Flash Point |
190.7±30.7 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
1.63
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
258
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C=C(C)C(NC2=NCCCS2)=C(C)C=1
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| InChi Key |
FXWQWFCVDXMJNM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H16N2OS/c1-8-6-10(15)7-9(2)11(8)14-12-13-4-3-5-16-12/h6-7,15H,3-5H2,1-2H3,(H,13,14)
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| Chemical Name |
4-(5,6-dihydro-4H-1,3-thiazin-2-ylamino)-3,5-dimethylphenol
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
Typically soluble in DMSO (e.g. 10 mM)
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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 | 4.2314 mL | 21.1569 mL | 42.3137 mL | |
| 5 mM | 0.8463 mL | 4.2314 mL | 8.4627 mL | |
| 10 mM | 0.4231 mL | 2.1157 mL | 4.2314 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.