| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Oxybutynin chloride (Ditropan; Ditropan XL), the hydrochloride salt of oxybutynin, is a competitive antagonist of muscarinic acetylcholine receptor subtypes M1, M2, and M3 used to treat bladder and urinary conditions (i.e. overactive bladder, urinary and bladder difficulties).
| Targets |
mAChR
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|---|---|
| ln Vitro |
In coronary artery smooth muscle cells, oxybutynin chloride (0.1, 0.3, 1, 3, 10, 30, 100 μM; 200 ms) inhibits vascular Kv channels in a concentration-dependent manner without causing an anticholinergic effect[1].
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| ln Vivo |
For specific [3H]N-methylscopolamine binding, 0.5 and 2 hours later, oxybutynin chloride (27.2 mg/kg; po; single) shows a 2-fold increase in Kd values[2]. This indicates a significant binding of mouse brain muscarinic receptors.
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| Enzyme Assay |
This study demonstrates the inhibitory effect of anticholinergic drug oxybutynin on voltage-dependent K+ (Kv) channels in rabbit coronary arterial smooth muscle cells. Oxybutynin inhibited vascular Kv channels in a concentration-dependent manner, with an IC50 value of 11.51 ± 0.38 μmol/L and a Hill coefficient (n) of 2.25 ± 0.12. Application of oxybutynin shifted the activation curve to the right and the inactivation curve to the left. Pretreatment with the Kv1.5 subtype inhibitor DPO-1 and the Kv2.1 subtype inhibitor guangxitoxin suppressed the oxybutynin-induced inhibition of the Kv current. However, application of the Kv7 subtype inhibitor linopirdine did not affect the inhibition by oxybutynin of the Kv current. The anticholinergic drug atropine did not inhibit the Kv current nor influence oxybutynin-induced inhibition of the Kv current. From these results, we concluded that oxybutynin inhibited the vascular Kv current in a concentration-dependent manner by influencing the steady-state activation and inactivation curves independent of its anticholinergic effect[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Coronary arterial smooth muscle cells (from Male New Zealand White rabbits) Tested Concentrations: 10 μM Incubation Duration: 200 ms Experimental Results: Rapidly inhibited the Kv current within 2 min and decreased the Kv current by 44% at +60 Mv. Inhibited the Kv current by changing the gating properties of Kv channels. Cell Viability Assay[1] Cell Types: Coronary arterial smooth muscle cells (from male New Zealand White rabbits) Tested Concentrations: 0.1, 0.3, 1, 3, 10, 30, 100 μM Incubation Duration: 200 ms Experimental Results: decreased the Kv current amplitude in a concentration-dependent manner, with an IC50 value of 11.51 μM. |
| Animal Protocol |
Animal/Disease Models: Male ddY strain mice (9 to 13weeks old)[2].
Doses: 27.2 mg/kg (76.1 µmol/kg) Route of Administration: Oral administration; single. Experimental Results: Significant increased Kd values for specific [3H]NMS binding in mouse bladder with values of 54.7% and 40.6% when at 0.5 and 2 hrs (hours), respectively. Significant increased Kd values for specific [3H]NMS binding in mouse cerebral cortex with values of 120% and 71.2% when at 0.5 and 2 hrs (hours), respectively. |
| References |
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| Additional Infomation |
Oxybutynin Chloride is the chloride salt form of oxybutynin, a tertiary amine and anticholinergic agent with antispasmodic activity. Oxybutynin chloride exerts its antimuscarinic effect on bladder smooth muscle by blocking muscarinic receptors in smooth muscle, thereby inhibiting acetylcholine binding. This results in a relaxation of bladder smooth muscle, a reduction of involuntary muscle contractions and delays the initial desire to void.
See also: Oxybutynin (has active moiety). |
| Molecular Formula |
C22H31NO3.HCL
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| Molecular Weight |
393.95
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| Exact Mass |
393.207
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| Elemental Analysis |
C, 67.07; H, 8.19; Cl, 9.00; N, 3.56; O, 12.18
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| CAS # |
1508-65-2
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| Related CAS # |
Oxybutynin;5633-20-5;(R)-Oxybutynin hydrochloride;1207344-05-5;Oxybutynin-d11 chloride;1185151-95-4;(R)-Oxybutynin;119618-21-2; 5633-20-5 (racemate); 1508-65-2 (racemate HCl); 1207344-05-5 (R-isomer HCl); 119618-21-2 (R-isomer); 2738613-22-2 (R-isomer citrate); 119618-22-3 (S-isomer); 2862851-81-6 (R-isomer tartrate); 230949-16-3 (S-isomer HCl)
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| PubChem CID |
91505
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| Appearance |
Typically exists as White to off-white solids at room temperature
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| Boiling Point |
494.4ºC at 760 mmHg
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| Melting Point |
126-128ºC
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| Vapour Pressure |
1.37E-10mmHg at 25°C
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| LogP |
4.144
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
27
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O([H])C(C(=O)OC([H])([H])C#CC([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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| InChi Key |
SWIJYDAEGSIQPZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H31NO3.ClH/c1-3-23(4-2)17-11-12-18-26-21(24)22(25,19-13-7-5-8-14-19)20-15-9-6-10-16-20;/h5,7-8,13-14,20,25H,3-4,6,9-10,15-18H2,1-2H3;1H
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| Chemical Name |
4-Diethylaminobut-2-ynyl 2-cyclohexyl-2-hydroxy-2-phenylethanoate Hydrochloride
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| Synonyms |
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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. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.35 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 (6.35 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 (6.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (253.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5384 mL | 12.6920 mL | 25.3839 mL | |
| 5 mM | 0.5077 mL | 2.5384 mL | 5.0768 mL | |
| 10 mM | 0.2538 mL | 1.2692 mL | 2.5384 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06181591 | Not yet recruiting | Drug: Mirabegron 50 MG Drug: Oxybutynin Chloride 5 MG |
Overactive Bladder | Seoul National University Hospital | April 1, 2024 | Phase 2 |
| NCT03187795 | Unknown † | Drug: Oxybutynin Chloride IR Drug: Mirabegron |
Spinal Cord Injuries Urinary Bladder, Neurogenic |
Kessler Foundation | April 3, 2019 | Phase 2 |
| NCT02099695 | Withdrawn | Drug: Oxybutynin Drug: Placebo |
Hyperhidrosis | Cristália Produtos Químicos Farmacêuticos Ltda. | December 2015 | Phase 3 |
| NCT02961790 | Completed Has Results | Drug: Oxybutynin Chloride Other: Placebo Other: Quality-of-Life Assessment Other: Questionnaire Administration |
Breast Carcinoma Ductal Breast Carcinoma In Situ Hot Flashes |
Academic and Community Cancer Research United |
December 9, 2016 | Phase 3 |
| NCT05637671 | Recruiting | Drug: oxybutynin ER Drug: Paroxetine CR |
Vasomotor Symptoms | Cairo University | February 10, 2022 | Phase 3 |
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