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| Targets |
CAS# 2673270-13-6. Tropicamide (parent compound) is a selective M4 muscarinic acetylcholine receptor antagonist. It blocks the muscarinic receptors in the iris sphincter muscle and ciliary muscle, leading to pupillary dilation (mydriasis) and paralysis of accommodation (cycloplegia). The M4 selectivity is a key feature, as it reduces the systemic side effects (e.g., tachycardia) associated with non‑selective antimuscarinics. Tropicamide-d3 has the same pharmacology but is used as an analytical standard.
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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].
Not applicable. Tropicamide-d3 itself is not used for measuring pharmacological activity. It is employed as an internal standard. The parent compound tropicamide, at concentrations of 0.5-1%, applied topically to the eye, produces mydriasis and cycloplegia within 15-30 minutes, lasting 4-6 hours. It has an IC₅0 in the low nanomolar range for M4 receptors and a short duration of action due to its relatively low lipophilicity and rapid clearance from the eye. |
| Enzyme Assay |
For analytical method development, Tropicamide-d3 is used as an internal standard. A stock solution is prepared in methanol or acetonitrile at 1 mg/mL. Calibration standards are prepared by spiking blank biological matrix (e.g., plasma, aqueous humor, urine) with known concentrations of unlabeled tropicamide (0.1-1000 ng/mL) and a fixed concentration of Tropicamide-d3 (50-100 ng/mL). Proteins are precipitated with 3‑5 volumes of acetonitrile containing the internal standard. After centrifugation, the supernatant is evaporated under nitrogen and reconstituted in mobile phase (0.1% formic acid in water/methanol). Analysis is performed by LC‑MS/MS in MRM mode, monitoring transitions m/z 285.2 → 240.2 for tropicamide and m/z 288.2 → 243.2 for Tropicamide-d3 (shift due to D3 label). The peak area ratio (analyte/IS) is plotted against the nominal concentration to generate a calibration curve.
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| Cell Assay |
Not applicable. Tropicamide-d3 is not used in cellular assays. The parent compound tropicamide, in cell systems expressing recombinant muscarinic receptors, can be used to study M4 receptor antagonism. Typically, M4‑expressing cells are used in calcium (if Galpha15 co‑expressed) or cAMP inhibition assays. Tropicamide would reverse agonist‑induced inhibition of cAMP with an IC₅0 in the low nanomolar range. However, the labeled compound is not used in functional assays.
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| Animal Protocol |
Tropicamide-d3 is used in ADME and bioequivalence studies. Animals (e.g., male Sprague‑Dawley rats, 200-300 g; rabbits for ophthalmic studies) or human subjects are administered tropicamide (e.g., 1-2 drops of a 0.5-1% ophthalmic solution). Blood, plasma, aqueous humor, or urine samples are collected at various time points (e.g., 0, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h). The concentration of tropicamide is measured by LC‑MS/MS using Tropicamide-d3 as an internal standard. Pharmacokinetic parameters (Cmax, Tmax, AUC, t½) are calculated by non‑compartmental analysis. In ocular pharmacokinetic studies, the aqueous humor is aspirated from the anterior chamber of the eye under anesthesia, and the concentration of tropicamide is measured. The labeled compound is also used to study the metabolism of tropicamide; it is primarily hydrolyzed to tropic acid by esterases in the plasma and liver.
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| ADME/Pharmacokinetics |
Tropicamide-d3 (MW 287.37, C17H17D3N2O2) is a stable isotope‑labeled compound with 99 atom% deuterium at the ethyl group (C2H5→CD3). It has the same chemical and physical properties as unlabeled tropicamide. Tropicamide is a lipophilic weak base (pKa ~5.7) that is well absorbed systemically through the conjunctiva and nasal mucosa after eye drop application. It has a plasma half‑life of approximately 30-60 minutes. It is metabolized primarily by esterases to tropic acid and other inactive metabolites. Less than 5% is excreted unchanged in urine. The deuterium label does not alter its pharmacokinetics.
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| Toxicity/Toxicokinetics |
Tropicamide-d3 is chemically stable and non‑toxic at the concentrations used as an internal standard (ng/mL levels). Unlabeled tropicamide is a clinically approved ophthalmic drug with a well‑characterized safety profile; adverse effects include transient stinging, blurred vision, photophobia, and rarely, systemic effects such as dry mouth, tachycardia, and confusion (particularly in children). The labeled analog has the same safety profile as the parent drug but is not used as a therapeutic agent; it is used only as an analytical standard.
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| References |
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| Additional Infomation |
Tropicamide-d3 (CAS 2673270-13-6) is a stable isotope‑labeled analog of tropicamide, a selective M4 muscarinic receptor antagonist and a short‑acting mydriatic/cycloplegic agent used in ophthalmic examinations. It is used as an internal standard for LC‑MS/MS quantification of tropicamide in biological samples. The parent compound is a clinically approved drug; the labeled analog is for research and analytical use only.
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| Exact Mass |
287.171
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| CAS # |
2673270-13-6
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| Related CAS # |
Tropicamide;1508-75-4
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| PubChem CID |
154731334
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
310
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])([2H])CN(CC1=CC=NC=C1)C(=O)C(CO)C2=CC=CC=C2
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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.) |
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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