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Midodrine hydrochloride (Amatine; Orvaten; Midodrine HCl; Pro-Amatine), the hydrochloride salt of midodrine which is a phenylalkanolamine derivative, is a potent adrenergic alpha-1 agonist that has been found to be able to increase arterial pressure, thus may be useful in managing hypotensive conditions owing to their long lasting blood pressure increasing effects.
Additional Infomation |
Midodrine hydrochloride is a hydrochloride resulting from the combination of equimolar amounts of midodrine and hydrogen chloride. Midodrine is a direct-acting sympathomimetic with selective alpha-adrenergic agonist activity. The hydrochloride salt is used as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine. It has a role as an alpha-adrenergic agonist, a sympathomimetic agent and a vasoconstrictor agent. It contains a midodrine(1+).
Midodrine Hydrochloride is the hydrochloride salt form of midodrine, a direct-acting prodrug and sympathomimetic agent with antihypotensive properties. Midodrine is converted to its active metabolite, desglymidodrine by deglycination reaction. Desglymidodrine selectively binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. This causes smooth muscle contraction and leads to an elevation of blood pressure. Desglymidodrine diffuses poorly across the blood-brain barrier, and is therefore not associated with effects on the central nervous system. An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION. See also: Midodrine (has active moiety). |
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Molecular Formula |
C12H19CLN2O4
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Molecular Weight |
290.74
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Exact Mass |
290.103
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CAS # |
43218-56-0
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Related CAS # |
Midodrine-d6 hydrochloride;1188265-43-1;Midodrine;42794-76-3
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PubChem CID |
18340
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Appearance |
White to yellow solid powder
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Boiling Point |
529.9ºC at 760 mmHg
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Flash Point |
274.3ºC
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LogP |
1.705
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Hydrogen Bond Donor Count |
4
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
6
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Heavy Atom Count |
19
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Complexity |
263
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Defined Atom Stereocenter Count |
0
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InChi Key |
MGCQZNBCJBRZDT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C12H18N2O4.ClH/c1-17-8-3-4-11(18-2)9(5-8)10(15)7-14-12(16)6-13;/h3-5,10,15H,6-7,13H2,1-2H3,(H,14,16);1H
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Chemical Name |
2-Amino-N-(2-(2,5-dimethoxyphenyl)-2-hydroxyethyl)acetamide monohydrochloride
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Synonyms |
Midodrine HCl Pro-Amatine Amatine OrvatenMidodrine hydrochloride
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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) |
H2O : ~100 mg/mL (~343.95 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 | 3.4395 mL | 17.1975 mL | 34.3950 mL | |
5 mM | 0.6879 mL | 3.4395 mL | 6.8790 mL | |
10 mM | 0.3439 mL | 1.7197 mL | 3.4395 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
Completed | NCT03129542 | Drug: Midodrine Hydrochloride 10 milligrams
Drug: Placebo capsule |
Blood Pressure Sepsis |
Mayo Clinic | 2017-08-30 | Phase 1 |
NCT00650013 | Completed | Drug: Midodrine HCl Tablets 5 mg Drug: ProAmatine® Tablets 5 mg |
Healthy | Mylan Pharmaceuticals Inc | 2002-07 | Phase 1 |
NCT00648440 | Completed | Drug: Midodrine HCl Tablets 5 mg Drug: ProAmatine® Tablets 5 mg |
Healthy | Mylan Pharmaceuticals Inc | 2002-10 | Phase 1 |
NCT00650364 | Completed | Drug: Midodrine HCl Tablets 5 mg Drug: ProAmatine® Tablets 5 mg |
Healthy | Mylan Pharmaceuticals Inc | 2002-08 | Phase 1 |
Completed WITH RESULTS | NCT00426842 | Drug: Midodrine Hydrochloride | Orthostatic Hypotension Spinal Cord Injury |
James J. Peters Veterans Affairs Medical Center | 2007-01 | Phase 2 |