| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Imidafenacin (formerly also known as KRP-197 and ONO-8025) is a novel, potent and selective inhibitor of M3 receptors with Kb of 0.317 nM and with less potency for M2 receptors (IC50 = 4.13 nM).
| Targets |
M3 receptor ( Ki = 0.3 nM ); M3 receptor ( Kd = 0.317 nM ); M2 receptor ( IC50 = 4.13 nM )
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|---|---|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The absolute oral bioavailability is 57.8%. Tmax is 1-3 h after administration. 10% is excreted in the urine as the parent compound. Most is eliminated by metabolism thought to be mediated by CYP3A4 and UGT1A4. The estimated volume of distribution is 43.9 L. The estimated clearance is 21.2 L/h. Metabolism / Metabolites Thought to be metabolized v by CYP3A4 and UGT1A4. No active metabolites have been observed. Biological Half-Life The half life of elimination is 3 h. |
| Toxicity/Toxicokinetics |
Protein Binding
Imidafenacin is 88% bounf by human plasma proteins. It binds to serum albumin and α1-acid glycoprotein. |
| References |
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| Additional Infomation |
Imidafenacin is a diarylmethane.
Imidafenacin is an antispasmodic agent with anticholinergic effects. It antagonizes muscarinic receptors in the bladder to reduce the frequency of urination in the treatment of overactive bladder. It is marketed in Japan under the tradenames Staybla by Ono Pharmaceutical and Uritos by Kyojin Pharmaceutical. Drug Indication Used in the treatment of overactive bladder. FDA Label Mechanism of Action Imidafenacin binds to and antagonizes muscarinic M1 and M3 receptors with high affinity. It also antagonizes muscarinic M2 receptors but with lower affinity. M3 receptors stimulate contraction of the detrusor muscle in the bladder via release of calcium from the sarcoplasmic reticulum. M2 receptors are also present in the detrusor muscle but serve to inhibit adenylate cyclase which reduces the relaxation mediated by β adrenergic receptors. Finally, M1 receptors are present on the parasympathetic neurons which release acetylcholine in the bladder. They act as an autocrine positive feedback loop and further increase release of acetylcholine. Antagonism of these receptors by imidafenacin prevents contraction of the bladder's detrusor muscle, prevents inhibition of the relation produced by sympathetic tone, and reduces acetylcholine release. Together these reduce the frequency of urination. Pharmacodynamics Imidafenacin is an antimuscarinic agent which acts to reduce the frequency of urination in patients with overactive bladder. |
| Molecular Formula |
C20H21N3O
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|---|---|
| Molecular Weight |
319.40024
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| Exact Mass |
319.168
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| Elemental Analysis |
C, 75.21; H, 6.63; N, 13.16; O, 5.01
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| CAS # |
170105-16-5
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| Related CAS # |
170105-16-5; 893421-54-0 (Imidafenacin HCl)
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| PubChem CID |
6433090
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
579.7±50.0 °C at 760 mmHg
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| Flash Point |
304.4±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.603
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| LogP |
2.42
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
395
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC(C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3C(C)=NC=C3)=O
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| InChi Key |
SQKXYSGRELMAAU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21N3O/c1-16-22-13-15-23(16)14-12-20(19(21)24,17-8-4-2-5-9-17)18-10-6-3-7-11-18/h2-11,13,15H,12,14H2,1H3,(H2,21,24)
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| Chemical Name |
4-(2-methylimidazol-1-yl)-2,2-diphenylbutanamide
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| Synonyms |
KRP-197; ONO-8025; KRP 197; ONO 8025; KRP197; ONO8025
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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: 31.3~63 mg/mL (97.8~197.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.51 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 20.8 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: ≥ 2.08 mg/mL (6.51 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 20.8 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: ≥ 2.08 mg/mL (6.51 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 | 3.1309 mL | 15.6544 mL | 31.3087 mL | |
| 5 mM | 0.6262 mL | 3.1309 mL | 6.2617 mL | |
| 10 mM | 0.3131 mL | 1.5654 mL | 3.1309 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 |
| NCT00212706 | Completed | Drug: ONO-8025 (KRP-197) | Overactive Bladder | Ono Pharmaceutical Co. Ltd | October 2001 | Phase 2 |
| NCT00212732 | Completed | Drug: ONO-8025 (KRP-197) | Overactive Bladder | Ono Pharmaceutical Co. Ltd | October 2003 | Phase 3 |
| NCT01578304 | Completed | Drug: Imidafenacin Drug: Fesoterodine |
Overactive Bladder | LG Life Sciences | December 2010 | Phase 4 |
| NCT00512785 | Completed | Drug: imidafenacin, KRP-197/ ONO-8025 |
Overactive Bladder | Ono Pharmaceutical Co. Ltd | August 2007 | Phase 3 |
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