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| Targets |
Iperoxo targets muscarinic acetylcholine receptors (mAChRs). It is a potent superagonist of these receptors. It stimulates [35S]GTPγS binding to CHO cell membranes expressing human M2 and M4 muscarinic receptors with EC50 values of 2.12 nM and 8.47 nM, respectively. Its potency at M2 and M4 receptors has been confirmed in functional assays.
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| ln Vitro |
Iperoxo is a potent superagonist of muscarinic acetylcholine receptors. It stimulates [35S]GTPγS binding to CHO cell membranes expressing human M2 and M4 muscarinic receptors with EC50 values of 2.12 nM and 8.47 nM, respectively. It significantly exceeds ACh in G protein signaling competence in CHO-hM2 cells.
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| ln Vivo |
Iperoxo is used as a research tool to study muscarinic receptor function and conformational transitions. Its superagonist activity makes it a valuable probe for investigating receptor activation mechanisms. It is not used as a therapeutic agent.
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| Enzyme Assay |
The primary in vitro assays for Iperoxo include radioligand binding assays to measure its affinity for muscarinic receptors. Functional assays measure its ability to stimulate [35S]GTPγS binding, which is a measure of G protein activation. Its EC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for Iperoxo involve treating cells expressing muscarinic receptors, such as CHO cells, with the compound and measuring its effects on receptor-mediated signaling. Its ability to stimulate G protein activation and downstream signaling pathways is assessed. These assays confirm its superagonist activity.
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| Animal Protocol |
In vivo animal experiments for Iperoxo are not detailed in the provided sources. As a research tool, it is primarily used in in vitro studies to investigate muscarinic receptor function. Its in vivo effects would depend on its ability to cross the blood-brain barrier and activate central muscarinic receptors.
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| ADME/Pharmacokinetics |
Iperoxo has a molecular weight of 324.16 g/mol and a molecular formula of C10H17IN2O2. It is a small molecule that is typically used as a research reagent. It is a potent superagonist of muscarinic acetylcholine receptors. It is also a reagent for click chemistry.
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| Toxicity/Toxicokinetics |
The toxicological profile of Iperoxo is not extensively detailed in the provided sources. As a research compound, it is not intended for human use. Standard safety precautions should be followed when handling. Its safety would need to be established through preclinical studies if it were to be developed for therapeutic applications.
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| References | |
| Additional Infomation |
See also: Iperoxo (Note moved to).
Iperoxo (Iperoxo iodide) is a potent superagonist of muscarinic acetylcholine receptors. It stimulates [35S]GTPγS binding to M2 and M4 receptors with EC50 values of 2.12 nM and 8.47 nM, respectively. It is used as a research tool to probe muscarinic receptor activation and conformational transitions. It is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C9H14N2O2
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|---|---|
| Molecular Weight |
182.219662189484
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| Exact Mass |
324.033
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| CAS # |
247079-84-1
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| PubChem CID |
46854806
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| Appearance |
White to off-white solid powder
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| Melting Point |
211.5 - 212.5 °C
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
278
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XWEOIAMCTHLJJB-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C10H17N2O2.HI/c1-12(2,3)7-4-5-8-13-10-6-9-14-11-10;/h6-9H2,1-3H3;1H/q+1;/p-1
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| Chemical Name |
4-(4,5-dihydro-1,2-oxazol-3-yloxy)but-2-ynyl-trimethylazanium;iodide
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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 : ~62.5 mg/mL (~192.81 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 | 5.4879 mL | 27.4394 mL | 54.8787 mL | |
| 5 mM | 1.0976 mL | 5.4879 mL | 10.9757 mL | |
| 10 mM | 0.5488 mL | 2.7439 mL | 5.4879 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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