| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Terodiline targets muscarinic acetylcholine receptors (mAChRs) and calcium channels. It is an M1-selective muscarinic receptor antagonist with Kb values of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3), and ileal muscle (M3), respectively. Terodiline is also a Ca²⁺ blocker. It blocks hERG current with an IC₅₀ of 375 nM.
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| ln Vitro |
In vitro, Terodiline has anticholinergic and calcium antagonist properties. It effectively reduces abnormal bladder contractions caused by detrusor instability. Terodiline blocks hERG current with an IC₅₀ of 375 nM. It blocks acetylcholine's effects on muscarinic receptors, leading to muscle relaxation.
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| ln Vivo |
Trodiline (80 mg/kg; SC) has an equivalent effect on pupil diameter (ED50 = 59 mg/kg) and inhibits intravesical bladder pressure and carbachol-induced salivation (ID50 = 24 and 35 mg/kg, respectively) [1].
In vivo, in Hartley guinea pigs weighing 200-600 g, Terodiline (80 mg/kg; subcutaneous administration) has an ID₅₀ of 24±6 mg/kg, with higher doses leading to death. Terodiline has been used in the study of disorders caused by detrusor instability and has potential for research in urinary incontinence. |
| Enzyme Assay |
Terodiline's receptor binding affinities can be characterized using radioligand binding assays in tissues such as rabbit vas deferens (M1), atria (M2), bladder (M3), and ileal muscle (M3). The compound has Kb values of 15, 160, 280, and 198 nM, respectively. hERG channel blockade can be assessed using electrophysiological assays.
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| Cell Assay |
In vitro cell experiments with Terodiline involve treating cells expressing muscarinic receptors or calcium channels with the compound and measuring receptor activity or calcium flux. The compound's effects on bladder smooth muscle contraction can be studied in tissue bath assays.
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| Animal Protocol |
Animal/Disease Models: Female or male Hartley guinea pig (200-600 g) [1]
Doses: 80 mg/kg Route of Administration: subcutaneous injection Experimental Results: Generated an ID50 of 24±6 mg/kg. Higher doses are fatal. In vivo animal studies with Terodiline have been conducted using Hartley guinea pigs. The compound is administered subcutaneously at 80 mg/kg to determine the ID₅₀ of 24±6 mg/kg. Higher doses lead to death. The compound's effects on bladder function and cardiovascular parameters can be assessed. |
| ADME/Pharmacokinetics |
Terodiline has a molecular weight of 281.44 and a molecular formula of C₂₀H₂₇N. The compound is stored as a powder at -20°C for 3 years or in solvent at -80°C for 1 year. It is soluble in DMSO (100 mg/mL). The compound is cardiotoxic due to hERG channel blockade.
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| Toxicity/Toxicokinetics |
Terodiline is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions due to its cardiotoxic properties.
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| References |
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| Additional Infomation |
Terodiline is a diarylmethane.
Terodiline is an antispasmodic agent that blocks hERG current with an IC₅₀ of 375 nM. It has both anticholinergic and calcium antagonist properties. Terodiline is an M1-selective muscarinic receptor antagonist with Kb values of 15, 160, 280, and 198 nM for M1, M2, and M3 receptors. |
| Molecular Formula |
C20H27N
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|---|---|
| Molecular Weight |
225.32900
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| Exact Mass |
225.152
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| CAS # |
15793-40-5
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| Related CAS # |
Terodiline hydrochloride;7082-21-5
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| PubChem CID |
23480
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| Appearance |
Typically exists as solid at room temperature
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| Density |
0.956g/cm3
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| Boiling Point |
390.9ºC at 760mmHg
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| Flash Point |
168.9ºC
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| Vapour Pressure |
2.57E-06mmHg at 25°C
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| Index of Refraction |
1.534
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| LogP |
4.256
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
261
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CC(C1=CC=CC=C1)C2=CC=CC=C2)NC(C)(C)C
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| InChi Key |
UISARWKNNNHPGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H27N/c1-16(21-20(2,3)4)15-19(17-11-7-5-8-12-17)18-13-9-6-10-14-18/h5-14,16,19,21H,15H2,1-4H3
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| Chemical Name |
N-tert-butyl-4,4-diphenylbutan-2-amine
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| Synonyms |
Terodiline; 15793-40-5; Terodilina; Terodilinum; N-tert-Butyl-1-methyl-3,3-diphenylpropylamine;
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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 | 4.4379 mL | 22.1897 mL | 44.3794 mL | |
| 5 mM | 0.8876 mL | 4.4379 mL | 8.8759 mL | |
| 10 mM | 0.4438 mL | 2.2190 mL | 4.4379 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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