| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Velufenacin specifically targets muscarinic acetylcholine receptors, with selectivity for the M3 receptor subtype. By blocking muscarinic receptor activity, it reduces parasympathetic nervous system signaling, leading to decreased smooth muscle contraction and glandular secretion. The compound demonstrates tissue selectivity for the urinary bladder over salivary glands.
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| ln Vitro |
In vitro, Velufenacin demonstrates significant biological activity in various cell-based models. As a muscarinic receptor antagonist, it blocks acetylcholine-induced receptor activation, thereby inhibiting downstream signaling pathways. The compound's selectivity for M3 receptors and tissue selectivity for bladder over salivary glands have been characterized in preclinical studies.
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| ln Vivo |
In vivo, Velufenacin has been evaluated in preclinical models for the treatment of overactive bladder. Its tissue selectivity for the urinary bladder over salivary glands suggests a favorable side-effect profile with reduced dry mouth compared to non-selective muscarinic antagonists. The compound has progressed to clinical trials for overactive bladder.
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| Enzyme Assay |
The binding affinity of Velufenacin to muscarinic receptor subtypes is assessed using radioligand binding assays. Membranes from cells expressing recombinant human M1-M5 muscarinic receptors are incubated with a radiolabeled antagonist (e.g., [³H]-NMS) in the presence of varying concentrations of the compound. IC50 or Ki values are calculated from competition binding curves to determine receptor subtype selectivity.
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| Cell Assay |
Cellular assays for Velufenacin involve the use of cells expressing recombinant muscarinic receptors. Receptor activation is measured by assessing intracellular calcium mobilization (for M1, M3, M5) or cAMP inhibition (for M2, M4). Cells are pre-incubated with the compound and then stimulated with a muscarinic agonist (e.g., carbachol or acetylcholine). The extent of receptor activation is quantified to determine antagonist potency.
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| Animal Protocol |
In vivo studies of Velufenacin are conducted in rodent models of overactive bladder. The compound is administered orally or intravenously. Bladder contractility is assessed using cystometry. Salivary secretion is measured to evaluate selectivity over salivary glands. Pharmacokinetic parameters are determined from plasma samples. The compound has been evaluated in clinical trials.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Velufenacin (molecular weight 362.83) are evaluated in preclinical species and in clinical trials. The compound is formulated for oral administration. Plasma concentrations are measured using LC-MS/MS to determine key PK parameters including oral bioavailability, half-life, and clearance. Tissue distribution studies assess bladder versus salivary gland exposure.
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| Toxicity/Toxicokinetics |
Velufenacin has been evaluated in clinical trials for overactive bladder. Standard preclinical toxicology assessments have been conducted as part of its development program. The compound's tissue selectivity suggests a favorable safety profile with reduced dry mouth side effects compared to non-selective muscarinic antagonists.
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| References | |
| Additional Infomation |
Velufenacin (DA-8010) is an investigational drug that has been studied in clinical trials for the treatment of overactive bladder. The compound's M3 receptor selectivity and tissue selectivity for bladder over salivary glands are designed to provide therapeutic efficacy with reduced side effects. By blocking muscarinic receptors in the bladder, it reduces detrusor muscle overactivity and improves urinary symptoms.
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| Molecular Formula |
C19H20CLFN2O2
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|---|---|
| Molecular Weight |
362.829
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| Exact Mass |
362.119
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| Elemental Analysis |
C, 62.90; H, 5.56; Cl, 9.77; F, 5.24; N, 7.72; O, 8.82
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| CAS # |
1648737-78-3
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| PubChem CID |
121425461
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
444.9±35.0 °C at 760 mmHg
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| Flash Point |
222.8±25.9 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.589
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
453
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=C(C([H])=C([H])C(=C1[H])C1=C([H])C([H])=C([H])C([H])=C1N([H])C(=O)OC([H])([H])[C@@]1([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])F
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| InChi Key |
SYBGVVSJNMTWCI-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C19H20ClFN2O2/c1-23-9-8-13(11-23)12-25-19(24)22-18-5-3-2-4-15(18)14-6-7-17(21)16(20)10-14/h2-7,10,13H,8-9,11-12H2,1H3,(H,22,24)/t13-/m1/s1
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| Chemical Name |
[(3R)-1-methylpyrrolidin-3-yl]methyl (3'-chloro-4'-fluoro[1,1'-biphenyl]-2-yl)carbamate
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| Synonyms |
Velufenacin
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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) |
DMSO : ~100 mg/mL (~275.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.89 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 (6.89 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 (6.89 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 | 2.7561 mL | 13.7806 mL | 27.5611 mL | |
| 5 mM | 0.5512 mL | 2.7561 mL | 5.5122 mL | |
| 10 mM | 0.2756 mL | 1.3781 mL | 2.7561 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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