| Targets |
MG 1 targets the α₁-adrenergic receptor, a G protein-coupled receptor that mediates the effects of norepinephrine and epinephrine. It acts as a selective antagonist. By blocking α₁-adrenergic receptors, it inhibits vascular smooth muscle contraction and modulates cardiovascular function.
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| ln Vitro |
See compound 23[1].
In vitro, MG 1 demonstrates potent antagonist activity at the α₁-adrenergic receptor. It has significant biological activity in modulating vascular smooth muscle contraction. It is a valuable tool for studying α₁-adrenergic receptor function. |
| ln Vivo |
In vivo, MG 1 has applications in studying cardiovascular function and related signal transduction pathways. By blocking α₁-adrenergic receptors, it modulates blood pressure and vascular tone.
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| Enzyme Assay |
The in vitro receptor binding assay for MG 1 involves competition binding experiments using radiolabeled α₁-adrenergic receptor ligands. Membranes from cells expressing α₁-adrenergic receptors are incubated with varying concentrations of MG 1 and a fixed concentration of radioligand. IC₅₀ values are calculated.
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| Cell Assay |
In vitro cell-based assays for MG 1 are performed using cells expressing α₁-adrenergic receptors, such as vascular smooth muscle cells. Cells are treated with MG 1, and α₁-adrenergic receptor-mediated signaling, such as calcium mobilization or contraction, is measured. The compound's antagonist activity is assessed by its ability to block agonist-induced responses.
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| Animal Protocol |
In vivo animal experiments for MG 1 have been conducted in rodent models of cardiovascular disease. Animals are administered the compound, and blood pressure and heart rate are measured. The compound's effects on vascular function and other cardiovascular parameters are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MG 1 have been characterized in preclinical species. Detailed PK parameters such as half-life, clearance, and bioavailability are determined from plasma concentration-time profiles.
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| Toxicity/Toxicokinetics |
Toxicological data for MG 1 are limited. In standard preclinical safety assessments, it would be evaluated for potential off-target effects and general toxicity. The compound is intended for research use only and not for therapeutic use in humans.
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| References |
[1]. Nowaczyk A, et al. QSAR studies on a number of pyrrolidin-2-one antiarrhythmic arylpiperazinyls. Med Chem Res. 2012 Mar;21(3):373-381.
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| Additional Infomation |
MG 1 is a selective α₁-adrenergic receptor antagonist that has been used as a tool to study cardiovascular function. It has applications in studying vascular smooth muscle contraction and related signal transduction pathways. It has not been approved for clinical use.
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| Exact Mass |
303.195
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|---|---|---|
| CAS # |
148274-76-4
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| Related CAS # |
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| PubChem CID |
3035813
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.18g/cm3
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| Boiling Point |
529.5ºC at 760mmHg
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| Flash Point |
274ºC
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| Vapour Pressure |
4.86E-12mmHg at 25°C
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| Index of Refraction |
1.58
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| LogP |
0.732
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AFBKGQPVUQUMRC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H25N3O2/c21-16(14-20-8-4-7-17(20)22)13-18-9-11-19(12-10-18)15-5-2-1-3-6-15/h1-3,5-6,16,21H,4,7-14H2
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| Chemical Name |
1-[2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl]pyrrolidin-2-one
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| Synonyms |
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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 |
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| 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) |
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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.) |
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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