| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Tarafenacin targets the M3 muscarinic receptor, a G protein-coupled receptor that mediates smooth muscle contraction, particularly in the bladder. It is a highly selective M3 receptor antagonist. It has a Ki of 0.19 nM for M3 and 200-fold selectivity over the M2 receptor. By blocking M3 receptors, it inhibits smooth muscle contraction.
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| ln Vitro |
Tarafenacin is a high-affinity M3 muscarinic receptor selective antagonist in vitro. It has a Ki of 0.19 nM for the M3 receptor. It exhibits 200-fold higher affinity for M3 than for the M2 receptor. Specific details on assay conditions and additional in vitro data are not extensively provided in the available literature.
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| ln Vivo |
In vivo activity of Tarafenacin is not extensively detailed. As a selective M3 receptor antagonist, it would be expected to inhibit smooth muscle contraction, particularly in the bladder, making it useful for treating overactive bladder. Specific in vivo efficacy data, including dosing regimens and animal models, are not provided in the available literature.
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| Enzyme Assay |
In vitro receptor binding assays for Tarafenacin involve measuring affinity for M3 and M2 muscarinic receptors. Membrane preparations from cells expressing recombinant M3 or M2 receptors are incubated with radiolabeled ligands and varying concentrations of Tarafenacin. Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is collected by filtration and quantified by scintillation counting. Ki values are calculated from competition curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing M3 muscarinic receptors are cultured and treated with Tarafenacin at various concentrations. Receptor antagonism is measured by assessing inhibition of agonist-induced calcium mobilization or other downstream signaling pathways. Cell viability is assessed using standard assays.
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| ADME/Pharmacokinetics |
Tarafenacin D-tartrate (CAS 1159101-48-0) has a molecular formula of C25H26F4N2O8 and a molecular weight of 558.48. It is a powder. It is soluble in DMSO: ≥100 mg/mL (~179.06 mM). For in vivo formulation, it can be prepared in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline. Powder can be stored at -20°C for 3 years.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Tarafenacin are not extensively provided. As an M3 receptor antagonist, it would be expected to have a safety profile related to muscarinic receptor modulation. The compound is for research use only and is not for human or clinical use. Standard toxicology assessments would be required for therapeutic development.
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| References |
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| Additional Infomation |
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist. It is extensively utilized in research focusing on overactive bladder and other disorders involving smooth muscle contraction. No approved therapeutic status is reported.
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| Molecular Formula |
C25H26F4N2O8
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|---|---|
| Molecular Weight |
558.48
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| Exact Mass |
558.163
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| CAS # |
1159101-48-0
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| Related CAS # |
Tarafenacin;385367-47-5
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| PubChem CID |
42622929
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| Appearance |
White to off-white solid powder
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| LogP |
2.295
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
697
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1CN2CCC1[C@H](C2)OC(=O)N(CC3=CC(=C(C(=C3)F)F)F)C4=CC(=CC=C4)F.[C@H]([C@@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
YJBKAMMKXVRSAI-CUCKRJOPSA-N
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| InChi Code |
InChI=1S/C21H20F4N2O2.C4H6O6/c22-15-2-1-3-16(10-15)27(11-13-8-17(23)20(25)18(24)9-13)21(28)29-19-12-26-6-4-14(19)5-7-26;5-1(3(7)8)2(6)4(9)10/h1-3,8-10,14,19H,4-7,11-12H2;1-2,5-6H,(H,7,8)(H,9,10)/t19-;1-,2-/m00/s1
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| Chemical Name |
[(3R)-1-azabicyclo[2.2.2]octan-3-yl] N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamate;(2S,3S)-2,3-dihydroxybutanedioic acid
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| Synonyms |
Tarafenacin D tartrate; Tarafenacin D-tartrate; Tarafenacin (D-tartrate)
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ≥ 100 mg/mL (~179.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7906 mL | 8.9529 mL | 17.9057 mL | |
| 5 mM | 0.3581 mL | 1.7906 mL | 3.5811 mL | |
| 10 mM | 0.1791 mL | 0.8953 mL | 1.7906 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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