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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
ATP-sensitive potassium (KATP) channels. U 37883A is a selective inhibitor of KATP channels, with a higher affinity for the SUR2 subtype over SUR1. By blocking these channels, it can modulate insulin secretion, vascular smooth muscle contraction, and neuronal excitability.
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| ln Vitro |
PNU-37883A blocked four different types of KATP channels in HEK-293 cells that were stably expressing Kir6.2/SUR1, Kir6.2/SUR2A, Kir6.2/SUR2B, or Kir6.1/SUR2B, albeit to different degrees. suppresses the putative Kir6.2/SUR2B (IC50 of 15 μM) and Kir6.1/SUR2B (IC50 of 6 μM) smooth muscle KATP channel types. At an IC50 of 5 μM, PNU-37883A strongly suppresses the current produced by expressing Kir6.2Δ26 by itself. The IC50 increases to 38 μM when Kir6.2Δ26 and SUR2B are produced simultaneously [1]. Phenylephrine- or potassium chloride-precontracted aortic rings exhibit concentration-dependent relaxation of agmatine (100 μM) upon exposure to PNU 37883 (0.1-10 nM) hydrochloride. Vascular tone is not changed by PNU 37883 (10 nM) hydrochloride therapy alone, albeit [3].
U 37883A potently inhibits KATP channel activity in vitro. In patch-clamp studies, it has been shown to block the current through KATP channels in various cell types, including pancreatic beta cells, vascular smooth muscle cells, and neurons. The compound's selectivity for SUR2 over SUR1 subtypes has been characterized. |
| ln Vivo |
In vivo, U 37883A has been studied for its effects on glucose homeostasis, blood pressure, and neurological function. It has been shown to increase insulin secretion and lower blood glucose levels in animal models. Its effects on vascular tone can lead to vasoconstriction and an increase in blood pressure. The compound's neurological effects are less well-characterized.
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| Enzyme Assay |
In vitro receptor binding assays for U 37883A involve measuring its affinity for KATP channels using radioligand binding techniques. Membranes from cells expressing the channels are incubated with radiolabeled ligands such as [3H]glibenclamide and increasing concentrations of U 37883A. Ki values are determined from competition binding curves.
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| Cell Assay |
In vitro cellular assays for U 37883A involve treating cells expressing KATP channels with the compound and measuring channel activity using patch-clamp electrophysiology or ion flux assays. The compound's ability to block KATP currents is assessed. Its effects on insulin secretion from pancreatic beta cells can also be measured.
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| Animal Protocol |
In vivo animal studies for U 37883A typically involve administration to rodent models to assess its effects on glucose homeostasis, blood pressure, or neurological function. Blood glucose levels, insulin levels, and blood pressure are measured. The compound's effects on seizure models or other neurological endpoints may also be evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for U 37883A is limited. As a research compound, its properties such as bioavailability, half-life, and tissue distribution have been characterized in preclinical studies. The compound is typically administered orally or intraperitoneally.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of U 37883A are limited. Its safety profile has been assessed in the context of its use as a research tool. The compound's mechanism of action suggests potential for hypoglycemia and other metabolic effects. Comprehensive toxicological evaluation is needed before any clinical development.
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| References |
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| Additional Infomation |
U 37883A is a selective inhibitor of ATP-sensitive potassium (KATP) channels. It has been used as a research tool to study the physiological and pathophysiological roles of KATP channels in insulin secretion, vascular tone, and neuronal excitability. Its selectivity for the SUR2 subtype over SUR1 makes it a valuable tool for studying the different roles of KATP channel subtypes.
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| Molecular Formula |
C21H36CLN3O
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|---|---|
| Molecular Weight |
381.989
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| Exact Mass |
381.255
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| CAS # |
57568-80-6
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| PubChem CID |
64392
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| Appearance |
White to off-white solid powder
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| Boiling Point |
474.1ºC at 760mmHg
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| Flash Point |
240.5ºC
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| LogP |
4.696
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
464
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FZALCKUJYZCDOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H35N3O.ClH/c1-2-4-19(5-3-1)22-20(24-6-8-25-9-7-24)23-21-13-16-10-17(14-21)12-18(11-16)15-21;/h16-19H,1-15H2,(H,22,23);1H
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| Chemical Name |
N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide;hydrochloride
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| Synonyms |
U-37883A; U37883A; U 37883A
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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. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.6179 mL | 13.0893 mL | 26.1787 mL | |
| 5 mM | 0.5236 mL | 2.6179 mL | 5.2357 mL | |
| 10 mM | 0.2618 mL | 1.3089 mL | 2.6179 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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