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| Targets |
Y-26763 targets ATP-sensitive potassium (KATP) channels (Kir6 channels). As a KATP channel opener, it promotes membrane hyperpolarization by increasing potassium ion efflux. This reduces cellular excitability and influences smooth muscle tone. KATP channel activation in pancreatic β-cells inhibits insulin release, while in vascular smooth muscle it causes vasodilation.
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| ln Vitro |
In vitro, Y-26763 activates KATP channel currents in isolated human β-cells when used at a concentration of 200 μM. It increases the frequency of KATP channel openings in the presence of ATP. As a KATP channel opener and active metabolite of Y-27152, it demonstrates potent channel-activating properties.
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| ln Vivo |
In vivo, Y-26763 is a long-acting K⁺ channel opener with antihypertensive effects in hypertensive rats and dogs. It has less tachycardic effect compared to other KATP openers. Its vasodilatory and antihypertensive properties make it a valuable tool for studying cardiovascular function and blood pressure regulation.
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| Enzyme Assay |
In vitro receptor/channel binding assays for Y-26763 are performed using electrophysiological techniques such as patch-clamp recordings in cells expressing KATP channels. Channel activity is measured in the presence of ATP and increasing concentrations of the compound. The frequency of channel openings and the magnitude of KATP currents are quantified.
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| Cell Assay |
In vitro cellular assays for Y-26763 are performed using isolated human pancreatic β-cells or vascular smooth muscle cells. Cells are treated with the compound, and KATP channel currents are measured using patch-clamp electrophysiology. Insulin release from β-cells is measured to assess the functional consequences of KATP channel activation.
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| Animal Protocol |
In vivo animal experiments for Y-26763 are conducted in hypertensive rat and dog models. A typical protocol involves administration of the compound via oral or intravenous routes, followed by measurement of blood pressure, heart rate, and other cardiovascular parameters. Antihypertensive efficacy is assessed by comparing blood pressure reduction between treated and control groups.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Y-26763 have been characterized in part. The compound has a molecular weight of 276.29 and molecular formula C₁₄H₁₆N₂O₄. Its IUPAC name is N-((3S,4R)-6-cyano-3-hydroxy-2,2-dimethylchroman-4-yl)-N-hydroxyacetamide. It is supplied with purity >98%. Further PK details are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Toxicological data for Y-26763 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
N-[(3S,4R)-6-cyano-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl]-N-hydroxyacetamide is a 1-benzopyran.
Y-26763 is a KATP channel opener and the active metabolite of Y-27152. It has antihypertensive effects in hypertensive rats and dogs with less tachycardia. It is used in cardiovascular research to study KATP channel function, vasodilation, and blood pressure regulation. This product is for research use only. |
| Molecular Formula |
C14H16N2O4
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|---|---|
| Molecular Weight |
276.292
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| Exact Mass |
276.111
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| CAS # |
127408-31-5
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| PubChem CID |
121878
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.36g/cm3
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| Boiling Point |
455.4ºC at 760mmHg
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| Flash Point |
229.2ºC
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| Vapour Pressure |
4.4E-09mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
1.368
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
442
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(=O)N([C@H]1[C@@H](C(OC2=C1C=C(C=C2)C#N)(C)C)O)O
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| InChi Key |
IWTCFIIOUXJOOV-OLZOCXBDSA-N
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| InChi Code |
InChI=1S/C14H16N2O4/c1-8(17)16(19)12-10-6-9(7-15)4-5-11(10)20-14(2,3)13(12)18/h4-6,12-13,18-19H,1-3H3/t12-,13+/m1/s1
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| Chemical Name |
N-[(3S,4R)-6-cyano-3-hydroxy-2,2-dimethyl-3,4-dihydrochromen-4-yl]-N-hydroxyacetamide
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| Synonyms |
Y26763; Y 26763; Y-26763
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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) |
1M NaOH : 27 mg/mL (~97.72 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 | 3.6194 mL | 18.0969 mL | 36.1939 mL | |
| 5 mM | 0.7239 mL | 3.6194 mL | 7.2388 mL | |
| 10 mM | 0.3619 mL | 1.8097 mL | 3.6194 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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