Tarafenacin D-tartrate
Based on 1 Customer Validation
Tarafenacin (SVT-40776) D-tartrate is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin D-tartrate does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin D-tartrate can be used in the research of overactive bladder.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.75%
- CAS No.: 1159101-48-0
- Formule: C25H26F4N2O8
- Masse moléculaire:558.48
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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HY-B0215
Acetylcysteine -
HY-B0151
Pregnenolone -
HY-76299
Galanthamine -
HY-17368
Rivastigmine -
HY-B0215R
Acetylcysteine (Standard) -
HY-17360
Tiotropium Bromide -
HY-B0267
Oxybutynin -
HY-B0569
Hexamethonium Bromide -
HY-A0024
Tolterodine -
HY-B0151R
Pregnenolone (Standard) -
HY-17440
Rocuronium Bromide -
HY-17465
Glycopyrrolate
Activité biologique
Description
IC50 & Target
[1]|
mAChR3 0.19 nM (Ki) |
In Vitro
Tarafenacin (3-1000 nmol/L; 60 min) D-tartrate potently inhibits carbachol-induced contractions in mouse isolated urinary bladder detrusor smooth muscle[1].
Tarafenacin (0.1-10 μmol/L; 60 min) D-tartrate inhibits Carbachol (HY-B1208)-induced negative chronotropism in mouse isolated atrial tissue, exhibiting a 199-fold functional selectivity for mouse urinary bladder over atrial tissue[1].
Tarafenacin (20 min) D-tartrate potently inhibits Carbachol-induced inositol phosphate accumulation in mouse bladder smooth muscle with a Ki of 0.19 nM, and shows 23-fold greater selectivity over mouse salivary glands[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DH female guinea pigs (250-300 g)[1]
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Dosage:1-3000 nmol/kg (Log dose)
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Administration:i.v.; cumulative bolus; 15 min between doses
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Result:Inhibited spontaneous bladder contractions in a dose-dependent manner, with an ED25 of 17.1 nmol/kg.
Did not affect arterial blood pressure at tested doses, resulting in a bladder versus vascular selectivity of more than 175-fold.
Chemical Information
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CAS No. 1159101-48-0
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Appearance Solid
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Masse moléculaire 558.48
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Formule C25H26F4N2O8
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Color White to off-white
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SMILES
O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4.O[C@@H]([C@@H](C(O)=O)O)C(O)=O
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Synonyms
SVT-40776 D-tartrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (179.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Salcedo C, et al. In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. Br J Pharmacol. 2009;156(5):807-817. [Content Brief]
[2].
Balsa D, et al. FUNCTIONAL BLADDER SELECTIVITY OF SVT-40776: A COMPARATIVE
STUDY.
[3]. Huang X, et al. Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation. J Phys Chem B. 2012;116(1):532-541. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7906 mL | 8.9529 mL | 17.9057 mL | 44.7644 mL |
| 5 mM | 0.3581 mL | 1.7906 mL | 3.5811 mL | 8.9529 mL | |
| 10 mM | 0.1791 mL | 0.8953 mL | 1.7906 mL | 4.4764 mL | |
| 15 mM | 0.1194 mL | 0.5969 mL | 1.1937 mL | 2.9843 mL | |
| 20 mM | 0.0895 mL | 0.4476 mL | 0.8953 mL | 2.2382 mL | |
| 25 mM | 0.0716 mL | 0.3581 mL | 0.7162 mL | 1.7906 mL | |
| 30 mM | 0.0597 mL | 0.2984 mL | 0.5969 mL | 1.4921 mL | |
| 40 mM | 0.0448 mL | 0.2238 mL | 0.4476 mL | 1.1191 mL | |
| 50 mM | 0.0358 mL | 0.1791 mL | 0.3581 mL | 0.8953 mL | |
| 60 mM | 0.0298 mL | 0.1492 mL | 0.2984 mL | 0.7461 mL | |
| 80 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5596 mL | |
| 100 mM | 0.0179 mL | 0.0895 mL | 0.1791 mL | 0.4476 mL |
Tarafenacin D-tartrate Related Classifications
HY-14825A Related Classifications
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Keywords
- Tarafenacin
- 1159101-48-0
- SVT-40776
- SVT40776
- SVT 40776
- mAChR
- M3 muscarinic receptor
- detrusor contractile activity
- bladder smooth muscle
- M2 muscarinic receptors
- inositol phosphate accumulation
- overactive bladder syndrome
- urinary tissue
- human M5 mAChR
- salivary gland M3 receptors
- cardiac tissue
- Inhibitor
- inhibitor
- inhibit