| Size | Price | Stock | Qty |
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| 1mg |
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| 10mg |
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| Other Sizes |
| Targets |
Droxidopa is a substrate for aromatic L-amino acid decarboxylase (AAAD/DDC), which converts it directly to norepinephrine in a single decarboxylation step, bypassing the need for dopamine β-hydroxylase. This increases norepinephrine availability in sympathetic nerve terminals and peripheral tissues, restoring adrenergic tone in neurogenic orthostatic hypotension.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Droxidopa itself has low intrinsic receptor activity and functions as a prodrug; its pharmacological activity depends on enzymatic conversion to norepinephrine, which then activates α- and β-adrenergic receptors. In vitro studies show that droxidopa effectively increases norepinephrine synthesis and release with activity typically in the low micromolar range, and the labelled analogue is used to trace the decarboxylation step by LC-MS/MS. |
| ln Vivo |
In vivo, droxidopa raises standing blood pressure in neurogenic orthostatic hypotension models and patients by restoring norepinephrine levels. The ¹³C₂,¹⁵N-labelled standard is used to quantify droxidopa and norepinephrine enrichment in plasma and tissue, enabling pharmacokinetic and metabolic flux analysis without contributing independent pharmacological effects.
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| Enzyme Assay |
AAAD activity toward droxidopa is measured by incubating the substrate with recombinant or tissue-derived AAAD in the presence of pyridoxal phosphate, terminating the reaction with acid, and quantifying norepinephrine formation by HPLC with electrochemical detection or LC-MS/MS. Labelled droxidopa allows simultaneous tracking of substrate consumption and product formation in a single analytical run.
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| Cell Assay |
Cellular conversion assays use catecholaminergic cells such as PC12 or SH-SY5Y incubated with droxidopa or labelled droxidopa, followed by measurement of intracellular norepinephrine and its metabolites by LC-MS/MS. Functional readouts may include adrenergic receptor–mediated calcium mobilization or norepinephrine release, and the labelled tracer enables discrimination between newly synthesized and pre-existing norepinephrine pools.
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| Animal Protocol |
In vivo studies use animal models of orthostatic hypotension or autonomic failure, with droxidopa administered orally or intravenously. Blood pressure, heart rate, and plasma norepinephrine are monitored, and the stable-isotope-labelled compound is used to trace conversion and distribution by LC-MS/MS, enabling correlation of systemic exposure with pressor response and norepinephrine enrichment in target tissues.
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| References |
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| Molecular Formula |
C9H12CLNO5
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|---|---|
| Molecular Weight |
252.627000808716
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| Exact Mass |
252.044
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| CAS # |
1329556-63-9
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| Related CAS # |
Droxidopa;23651-95-8
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| PubChem CID |
131667937
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| Appearance |
Typically exists as solid at room temperature
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| tPSA |
124
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
235
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1=CC(=C(C=C1[C@H]([13C@@H]([13C](=O)O)[15NH2])O)O)O.Cl
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| InChi Key |
FFEWFMCABUNGJJ-OPABSIBTSA-N
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| InChi Code |
InChI=1S/C9H11NO5.ClH/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);1H/t7-,8+;/m0./s1/i7+1,9+1,10+1;
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| Chemical Name |
(2S,3R)-2-(15N)azanyl-3-(3,4-dihydroxyphenyl)-3-hydroxy(1,2-13C2)propanoic acid;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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.9584 mL | 19.7918 mL | 39.5836 mL | |
| 5 mM | 0.7917 mL | 3.9584 mL | 7.9167 mL | |
| 10 mM | 0.3958 mL | 1.9792 mL | 3.9584 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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