| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
α2-adrenoceptor (potent antagonist, pKi = 6.28). It has 7.4-fold higher affinity for α2-adrenergic receptors than for α1-adrenergic receptors.
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|---|---|
| ln Vitro |
Midaglizole (DG-5128) more effectively inhibits [3H]clonidine binding in rat cerebral cortical membranes at concentrations up to 10 μM than [3H]prazosin binding. The simple law of mass action is followed by the uniform suppression pattern [1]. Midagazole's EC50 values for inducing insulin release from MIN6 beta cell lines and rat pancreatic islets are 200 nM and 24 μM, respectively. For Kir6.2 and Kir6.2/SUR1, the IC50 values of midagazole-induced inhibition of KATP current are 3.8 μM and 4.4 uM, respectively [2].
In vitro, Midaglizole hydrochloride is a potent α2-adrenoceptor antagonist with pKi = 6.28 for α2 receptors. It has 7.4-fold higher affinity for α2 than α1 receptors. Quantitative IC50 values are not detailed in publicly available sources. |
| ln Vivo |
Rats' blood pressure rises when given intravenously 3 and 30 mg/kg of midaglitazole [3].
In vivo, Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats. It has been investigated as an antihypertensive and insulin-sensitizing agent. Detailed dose-response and pharmacokinetic data are limited. |
| Enzyme Assay |
No specific cell-free α2-adrenoceptor binding assay protocol is detailed for Midaglizole hydrochloride. For adrenergic receptor antagonists, typical cell-free assays include radioligand binding studies using [3H]rauwolscine or [3H]clonidine and membrane preparations from tissues expressing α2 receptors. pKi values are calculated from competition binding curves.
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| Cell Assay |
Cellular α2-adrenoceptor antagonism is assessed in cells expressing α2 receptors (e.g., inhibition of agonist-induced cAMP accumulation or calcium mobilization). Cells are treated with Midaglizole hydrochloride and stimulated with an α2 agonist; inhibition of the response is measured.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of hypertension or metabolic syndrome. Midaglizole hydrochloride is administered via intravenous or intraperitoneal injection. Endpoints include blood pressure, heart rate, glucose tolerance, and insulin sensitivity.
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| ADME/Pharmacokinetics |
Molecular weight: 324.25 g/mol; molecular formula: C16H19Cl2N3 (or C17H21N3 for the free base). Purity: typically >98%. CAS No.: 79689-25-1. Solubility: soluble in DMSO. Storage: -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As an α2-adrenoceptor antagonist, potential side effects may include cardiovascular effects (increased blood pressure). Standard toxicological studies would be required for drug development.
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| References |
[1]. Yamanaka K, et al. The selectivity of DG-5128 as an alpha 2-adrenoceptor antagonist. Eur J Pharmacol. 1984 Nov 27;106(3):625-8.
[2]. Proks P, et al. Inhibition of recombinant K(ATP) channels by the antidiabetic agents midaglizole, LY397364 and LY389382. Eur J Pharmacol. 2002 Sep 27;452(1):11-9. [3]. Hirohashi M, et al. Intrinsic pressor activity of midaglizole, an alpha-2 adrenoceptor antagonist, in pithed rats. Jpn J Pharmacol. 1990 Aug;53(4):519-20 |
| Additional Infomation |
See also: Midagliflozin (note moved to).
Midaglizole hydrochloride is a research-grade compound, not approved for therapeutic use. It is primarily used as a pharmacological tool for studying α2-adrenoceptor function, cardiovascular regulation, and insulin-modulating mechanisms. No clinical trials have been reported. Its mechanism involves α2-adrenoceptor antagonism. |
| Molecular Formula |
C₁₆H₁₉CL₂N₃
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|---|---|
| Molecular Weight |
324.25
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| Exact Mass |
323.096
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| CAS # |
79689-25-1
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| Related CAS # |
Midaglizole;66529-17-7
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| PubChem CID |
157562
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| Appearance |
White to off-white solid powder
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| Boiling Point |
460ºC at 760 mmHg
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| Flash Point |
232ºC
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| LogP |
3.973
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1=CC=CC=C1)(C2=CC=CC=N2)CC3=NCCN3.[2 HCl]
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| InChi Key |
PAKRIOPMNVCTCL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17N3.2ClH/c1-2-6-13(7-3-1)14(12-16-18-10-11-19-16)15-8-4-5-9-17-15;;/h1-9,14H,10-12H2,(H,18,19);2*1H
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| Chemical Name |
2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine;dihydrochloride
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| Synonyms |
DG5128; (±-DG5128
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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) |
DMSO : ~500 mg/mL (~1542.02 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 | 3.0840 mL | 15.4202 mL | 30.8404 mL | |
| 5 mM | 0.6168 mL | 3.0840 mL | 6.1681 mL | |
| 10 mM | 0.3084 mL | 1.5420 mL | 3.0840 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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