| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The molecular targets are muscarinic acetylcholine receptors, with pilocarpine acting as a partial agonist; it shows highest potency at M3 receptors (EC50 approximately 1 μM, 39% efficacy in some assays) and binds M1 receptors with IC50 approximately 4.43 μM in radioligand displacement assays, with weaker activity at other subtypes and no significant nicotinic receptor affinity.
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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].
In vitro, pilocarpine-d3 HCl activates M3 receptor–mediated calcium mobilization and phosphoinositide hydrolysis in transfected cells and isolated smooth muscle preparations, with EC50 values in the low micromolar range and partial agonist efficacy relative to carbachol; it stimulates secretion in salivary acinar cells and contracts iris sphincter preparations, and the deuterated form retains muscarinic agonist activity. |
| ln Vivo |
In vivo, oral or systemic pilocarpine-d3 HCl increases salivary and lacrimal secretion, reduces intraocular pressure, and induces cholinergic seizures in rodents at higher doses; it crosses the blood–brain barrier and activates central muscarinic receptors, and the labeled form is used to quantify plasma and tissue exposure and to relate muscarinic occupancy to secretory and convulsant effects.
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| Enzyme Assay |
Noncellular binding assays incubate membrane homogenates expressing recombinant human M1–M5 receptors or native tissues with [3H]N-methylscopolamine and increasing concentrations of pilocarpine-d3; agonist displacement curves are used to derive Ki values, and functional [35S]GTPγS binding assays quantify partial agonist efficacy at each subtype.
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| Cell Assay |
Cellular assays use CHO or HEK293 cells expressing M3 receptors and measure pilocarpine-d3–stimulated intracellular calcium mobilization or inositol phosphate accumulation; salivary acinar cells are used to measure amylase secretion, and isolated iris sphincter or ileum preparations are used to record contractile responses and derive EC50 values.
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| Animal Protocol |
Animal protocols administer pilocarpine-d3 HCl orally, intraperitoneally, or topically to mice or rats at doses of 1–50 mg/kg; salivary flow, lacrimal secretion, intraocular pressure, and seizure latency are measured, and plasma and brain concentrations are quantified by LC-MS/MS to relate muscarinic agonist exposure to secretory and central nervous system effects.
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| References |
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| Molecular Formula |
C11H17CLN2O2
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|---|---|
| Molecular Weight |
247.736366987228
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| Exact Mass |
247.116
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| CAS # |
1217838-88-4
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| Related CAS # |
Pilocarpine Hydrochloride;54-71-7
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| PubChem CID |
46782754
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| Appearance |
Typically exists as solid at room temperature
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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 |
3
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| Heavy Atom Count |
16
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| Complexity |
245
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| Defined Atom Stereocenter Count |
2
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| SMILES |
[2H]C([2H])([2H])N1C=NC=C1C[C@H]2COC(=O)[C@H]2CC.Cl
|
| InChi Key |
RNAICSBVACLLGM-ALOYQDBRSA-N
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| InChi Code |
InChI=1S/C11H16N2O2.ClH/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2;/h5,7-8,10H,3-4,6H2,1-2H3;1H/t8-,10-;/m0./s1/i2D3;
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| Chemical Name |
(3S,4R)-3-ethyl-4-[[3-(trideuteriomethyl)imidazol-4-yl]methyl]oxolan-2-one;hydrochloride
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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 | 4.0365 mL | 20.1824 mL | 40.3649 mL | |
| 5 mM | 0.8073 mL | 4.0365 mL | 8.0730 mL | |
| 10 mM | 0.4036 mL | 2.0182 mL | 4.0365 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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