| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Amlodipine-d4 targets the same biological targets as amlodipine. Amlodipine is a dihydropyridine calcium channel blocker that inhibits calcium ion influx by blocking voltage-dependent L-type calcium channels. As a deuterated compound, its primary use is as an analytical standard for pharmacokinetic studies and drug metabolism research.
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|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers that influence measurement during the drug development process. It's possible that the pharmacokinetics and functional range of medications contribute to the concern over mutagenesis [1].
Amlodipine-d4 itself is not evaluated for traditional in vitro biological activity. Its "activity" is as an analytical standard for the quantification of amlodipine in pharmacokinetic and drug metabolism studies. The unlabeled amlodipine is a calcium channel blocker. The deuterated version is used primarily as an internal standard. |
| ln Vivo |
Amlodipine-d4 is not administered as a therapeutic agent in vivo. Its primary application is as an analytical standard for the quantification of amlodipine. The compound is used in laboratory settings to measure the concentration of amlodipine in biological samples. It is not used in animal models as an active treatment.
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| Enzyme Assay |
Amlodipine-d4 is used as an internal standard in analytical chemistry. Its performance is assessed by its ability to provide accurate and precise quantification of amlodipine in complex matrices. The compound is typically analyzed by LC-MS/MS. Its isotopic purity and chemical purity are critical parameters for its use as an internal standard.
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| Cell Assay |
Amlodipine-d4 is used as an internal standard in the analysis of biological samples. It is added to samples containing amlodipine to correct for variability in sample preparation and instrument performance. The labeled and unlabeled compounds are co-eluted and detected by mass spectrometry, allowing for accurate quantification of amlodipine.
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| Animal Protocol |
Amlodipine-d4 is used in pharmaceutical research as an internal standard for the quantification of amlodipine in biological samples. It is added to samples from patients or animals to accurately measure amlodipine concentrations for pharmacokinetic and bioequivalence studies. The compound itself is not administered to animals.
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| ADME/Pharmacokinetics |
Amlodipine-d4 has a molecular weight of 412.90 g/mol and a molecular formula of C20H21D4ClN2O5. It is a deuterated form of amlodipine. The compound is typically stored at 2-8°C in a refrigerator or at -20°C for long-term storage. It is soluble in DMSO and other organic solvents. Amlodipine is an orally bioactive dihydropyridine calcium channel blocker.
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| Toxicity/Toxicokinetics |
Toxicological data for Amlodipine-d4 are not extensively detailed, as it is a research compound. It is not intended for human or veterinary use. Standard laboratory safety precautions, including the use of personal protective equipment (PPE), should be followed when handling the compound.
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| References |
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| Additional Infomation |
Amlodipine-d4 is a deuterated form of amlodipine, a widely used calcium channel blocker for the treatment of hypertension and angina. It can be used for analytical method development, method validation (AMV), Quality Controlled (QC) application for Abbreviated New Drug Application (ANDA) or during commercial production of Amlodipine. It is not approved for therapeutic use.
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| Molecular Formula |
C20H21D4CLN2O5
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|---|---|
| Molecular Weight |
412.90
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| Exact Mass |
412.17
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| CAS # |
1185246-14-3
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| Related CAS # |
Amlodipine;88150-42-9
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| PubChem CID |
45358917
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| Appearance |
White to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
527.2±50.0 °C at 760 mmHg
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| Melting Point |
131-133°C
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| Flash Point |
272.6±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.546
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| LogP |
4.16
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
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| Complexity |
647
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])(C([2H])([2H])OCC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC=CC=C2Cl)C(=O)OCC)N
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| InChi Key |
HTIQEAQVCYTUBX-YQUBHJMPSA-N
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| InChi Code |
InChI=1S/C20H25ClN2O5/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21/h5-8,17,23H,4,9-11,22H2,1-3H3/i9D2,10D2
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| Chemical Name |
3-O-ethyl 5-O-methyl 2-[(2-amino-1,1,2,2-tetradeuterioethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
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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 | 2.4219 mL | 12.1095 mL | 24.2189 mL | |
| 5 mM | 0.4844 mL | 2.4219 mL | 4.8438 mL | |
| 10 mM | 0.2422 mL | 1.2109 mL | 2.4219 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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