Size | Price | Stock | Qty |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Other Sizes |
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Purity: ≥98%
Oxybutynin (Ditropan, Lyrinel XL, Lenditro, Oxybutynin, Uripan) is a potent and competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties. Oxybutynin N-deethylation in human liver microsomes in vitro is potently inhibited by ketoconazole (IC50 4.5 mM), less and variably by itraconazole and not by quinidine or several other reference inhibitors, suggesting that CYP3A enzymes are predominant catalysts of the reaction.
ln Vitro |
In coronary artery smooth muscle cells, oxybutynin (0.1, 0.3, 1, 3, 10, 30, 100 μM; 200 ms) inhibits vascular Kv channels in a concentration-dependent manner without affecting the anticholinergic effect[1].
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ln Vivo |
When specific [3H]N-methylscopolamine binding occurs 0.5 and 2 hours later, oxybutynin (27.2 mg/kg; po; single) significantly binds mouse brain muscarinic receptors, increasing Kd values by about a factor of two[2].
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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 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 |
[1]. Li H, et al. The anticholinergic drug oxybutynin inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells. Clin Exp Pharmacol Physiol. 2019 Nov;46(11):1030-1036.
[2]. Oki T, et al. Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder. J Urol. 2007 Feb;177(2):766-70. |
Molecular Formula |
C22H31NO3
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Molecular Weight |
357.49
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CAS # |
5633-20-5
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Related CAS # |
Oxybutynin chloride;1508-65-2;(R)-Oxybutynin hydrochloride;1207344-05-5;(R)-Oxybutynin;119618-21-2
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SMILES |
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 |
XIQVNETUBQGFHX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H31NO3/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
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Chemical Name |
4-(diethylamino)but-2-ynyl 2-cyclohexyl-2-hydroxy-2-phenylacetate
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7973 mL | 13.9864 mL | 27.9728 mL | |
5 mM | 0.5595 mL | 2.7973 mL | 5.5946 mL | |
10 mM | 0.2797 mL | 1.3986 mL | 2.7973 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.