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Purity: ≥98%
Droxidopa (also known as L-DOPS; LDOPS; SM 5688; SM-5688; Northera; L-threodihydroxyphenylserine) is a potent psychoactive drug that acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline). Droxidopa is a prodrug that resembles noradrenaline structurally but has a carboxyl group. Unlike noradrenaline, dopa decarboxylase converts dopa after absorption into noradrenaline, increasing levels of the neurotransmitter that is identical to endogenous noradrenaline. This means that dopa can be given orally. The drug dronapa is well accepted.
| Targets |
Adrenergic Receptor
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| ln Vitro |
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| ln Vivo |
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| Animal Protocol |
250-380g male Sprague-Dawley rats
200 mg/kg (10 mg/kg, i.p. benserazide was given to the animals at 20 or 30 min prior to L-DOPS injection) I.p. |
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| References |
| Molecular Formula |
C9H11NO5
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|---|---|
| Molecular Weight |
213.19
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| Exact Mass |
213.06
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| Elemental Analysis |
C, 50.70; H, 5.20; N, 6.57; O, 37.52
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| CAS # |
23651-95-8
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| Related CAS # |
Droxidopa hydrochloride; 1260173-94-1; Droxidopa-13C2,15N hydrochloride; 1329556-63-9
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=C(C=C1[C@H]([C@@H](C(=O)O)N)O)O)O
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| InChi Key |
QXWYKJLNLSIPIN-JGVFFNPUSA-N
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| InChi Code |
InChI=1S/C9H11NO5/c10-7(9(14)15)8(13)4-1-2-5(11)6(12)3-4/h1-3,7-8,11-13H,10H2,(H,14,15)/t7-,8+/m0/s1
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| Chemical Name |
(2S,3R)-2-amino-3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid
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| Synonyms |
SM-5688; SM5688; SM 5688; Droxidopa; trade name: LDOPS; Northera; L-threodihydroxyphenylserine
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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) |
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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 | 4.6907 mL | 23.4533 mL | 46.9065 mL | |
| 5 mM | 0.9381 mL | 4.6907 mL | 9.3813 mL | |
| 10 mM | 0.4691 mL | 2.3453 mL | 4.6907 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 |
| NCT02558972 | Active Recruiting |
Drug: Placebo Drug: Northera (Droxidopa) |
Fainting Vasovagal Syncope (VVS) |
New York Medical College | September 2015 | Phase 2 |
| NCT02897063 | Recruiting | Drug: Droxidopa Drug: Midodrine Drug: Placebo |
Autonomic Failure Parkinson Disease |
Vanderbilt University Medical Center |
September 2016 | Phase 1 |
| NCT04977388 | Recruiting | Drug: Droxidopa Other: Placebo |
Alcohol Use Disorder Occipital Horn Syndrome |
Stephen G. Kaler, MD | July 12, 2021 | Phase 1 Phase 2 |
| NCT03173781 | Completed | Drug: droxidopa Drug: Placebo |
Parkinson's Disease | Colorado Springs Neurological Associates |
April 2016 | Not Applicable |
| NCT03602014 | Completed | Drug: Placebo Drug: Northera |
Hypotension, Orthostatic Spinal Cord Injuries Hypotension |
James J. Peters Veterans Affairs Medical Center |
June 1, 2018 | Phase 4 |
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