| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
ZM-226600 targets ATP-sensitive potassium channels (KATP), specifically Kir6 channels, which play critical roles in regulating cellular excitability. It is a potent KATP channel opener with an EC50 of 0.5 μM. By opening KATP channels, ZM-226600 hyperpolarizes cell membranes, reducing excitability in smooth muscle cells. This mechanism underlies its effects on bladder smooth muscle, making it effective for reducing overactive bladder.
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| ln Vitro |
ZM226600 (1 μM, 30 minutes) inhibits vaginal action automatically [1].
In vitro, ZM-226600 is a potent Kir6 (KATP) channel opener with an EC50 of 0.5 μM. It lacks anti-androgenic properties, distinguishing it from some other KATP openers. These in vitro properties make ZM-226600 a valuable tool for studying KATP channel function and its role in smooth muscle physiology. |
| ln Vivo |
ZM226600 (10-1000 nmol/kg, intravenously) does not considerably alter heart rate when under anesthesia [1].
In vivo, ZM-226600 is more effective than oxybutynin in reducing overactive bladder and does not have the vascular side effects observed with pinacidil. It has an inhibitory effect on spontaneous bladder activity. Its short duration of action (approximately 1 hour) may be a limitation for some applications. These in vivo effects support its potential for treating overactive bladder and other conditions involving smooth muscle hyperexcitability. |
| Enzyme Assay |
The in vitro receptor binding/ion channel assay for ZM-226600 involves measuring its effects on KATP channel activity. This can be assessed using patch-clamp electrophysiology in cells expressing KATP channels (e.g., Kir6.2/SUR1 or Kir6.1/SUR2B). The compound is applied at various concentrations, and channel activity is measured as changes in membrane potential or current. The EC50 for channel opening is calculated from dose-response curves. Radioligand binding assays with labeled KATP channel modulators can also be used to assess binding affinity.
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| Cell Assay |
The in vitro cell-based assay for ZM-226600 involves culturing smooth muscle cells (e.g., bladder smooth muscle cells) and treating them with the compound to assess effects on cell excitability and contraction. Cells are treated with ZM-226600 at various concentrations, and membrane potential is measured using fluorescent membrane potential dyes or patch-clamp electrophysiology. Smooth muscle contraction can be assessed using tissue bath experiments with isolated bladder strips. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for ZM-226600 have been conducted in models of overactive bladder. Rats or other animals are administered ZM-226600 orally or intravenously, and bladder function is assessed using cystometry or by measuring voiding behavior. The compound's effects on bladder activity, blood pressure, and other physiological parameters are monitored. Standard protocols for overactive bladder models are employed.
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| ADME/Pharmacokinetics |
ZM-226600 is a short-acting compound with a duration of action of approximately 1 hour. It has a molecular weight of 373.35 and a molecular formula of C16H14F3NO4S. The compound is soluble in DMSO (up to 100 mM) and can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are available from preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of ZM-226600 has been evaluated in preclinical studies. Unlike some other KATP channel openers, ZM-226600 does not have the vascular side effects observed with pinacidil, suggesting a more favorable cardiovascular safety profile. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents and dogs, with endpoints including clinical signs, body weight, clinical pathology, and histopathology.
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| References |
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| Additional Infomation |
N-[4-(benzenesulfonyl)phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropionamide is an aniline compound.
ZM-226600 is a research compound and has not been approved for clinical use. It is a potent and selective KATP channel opener with an EC50 of 0.5 μM. ZM-226600 is short-acting, lacks anti-androgenic properties, and is more effective than oxybutynin in reducing overactive bladder without the vascular side effects of pinacidil. It is a valuable tool for studying KATP channel function and bladder physiology. |
| Molecular Formula |
C16H14F3NO4S
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| Molecular Weight |
373.346
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| Exact Mass |
373.06
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| Elemental Analysis |
C, 51.47; H, 3.78; F, 15.27; N, 3.75; O, 17.14; S, 8.59
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| CAS # |
147695-92-9
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| PubChem CID |
5240098
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| Appearance |
White to off-white solid powder
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| Density |
1.448g/cm3
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| Boiling Point |
574.8ºC at 760 mmHg
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| Flash Point |
301.4ºC
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| Vapour Pressure |
4.72E-14mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
3.925
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
573
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C(=O)NC1=CC=C(C=C1)S(=O)(=O)C2=CC=CC=C2)(C(F)(F)F)O
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| InChi Key |
LJLXQHHFAKVTNP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14F3NO4S/c1-15(22,16(17,18)19)14(21)20-11-7-9-13(10-8-11)25(23,24)12-5-3-2-4-6-12/h2-10,22H,1H3,(H,20,21)
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| Chemical Name |
N-(4-Phenylsulfonylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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| Synonyms |
ZM-226600; ZM 226600; ZM226600;
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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 : ~250 mg/mL (~669.61 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6785 mL | 13.3923 mL | 26.7845 mL | |
| 5 mM | 0.5357 mL | 2.6785 mL | 5.3569 mL | |
| 10 mM | 0.2678 mL | 1.3392 mL | 2.6785 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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