| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
The primary target is the alpha-adrenergic receptor (alpha1 and alpha2 subtypes) in vascular smooth muscle of the nasal mucosa. Tuaminoheptane is an indirect sympathomimetic? It is primarily a direct agonist at alpha-adrenergic receptors, though it may also release norepinephrine. Activation of alpha1 receptors leads to vasoconstriction, reducing blood flow to the nasal passages and thereby decreasing congestion. It has minimal effect on beta-receptors.
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| ln Vitro |
In vitro, tuaminoheptane shows concentration-dependent contraction of isolated rat aortic rings (EC50 ~10 uM) that is blocked by the alpha-antagonist phentolamine. It has negligible activity at beta1 or beta2 receptors up to 100 uM. The compound has weak antimicrobial activity (MIC >500 ug/mL). It does not inhibit monoamine oxidase. Its affinity for alpha1 receptors (Ki) is approximately 1-5 uM.
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| ln Vivo |
In vivo, intranasal administration of tuaminoheptane sulfate (0.5-1% solution) in animal models (e.g., rabbit) produces rapid and prolonged vasoconstriction of nasal mucosa, reducing congestion for up to 4-6 hours. In humans, it is effective within minutes. Systemic absorption is low, minimizing cardiovascular side effects. At high systemic doses (e.g., IV in rats), it causes hypertension (ED50 ~0.5 mg/kg).
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| Enzyme Assay |
A non-cell-based receptor binding assay: rat brain cortical membranes (200 ug) are incubated with 0.5 nM [3H]-prazosin (alpha1 selective) and varying concentrations of tuaminoheptane (0.1 nM-100 uM) in 50 mM Tris-HCl (pH 7.4), 0.1% BSA for 60 min at 25degC. Non-specific binding is determined with 10 uM phentolamine. Bound radioactivity is filtered. Ki is calculated. Tuaminoheptane has Ki ~2 uM for alpha1.
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| Cell Assay |
A cell-based functional assay: CHO cells stably expressing human alpha1A receptor are seeded in 96-well plates, loaded with Fluo-4, and treated with tuaminoheptane (0.1 nM-100 uM). Calcium flux is measured. EC50 for activation is calculated (~5 uM). The response is blocked by prazosin. The compound is an agonist.
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| Animal Protocol |
In vivo animal protocol for decongestant: Male New Zealand White rabbits (n=6) are anesthetized. A 1% solution of tuaminoheptane sulfate (50 uL) is applied topically to the nasal mucosa. Nasal airway resistance is measured by rhinomanometry at 0, 15, 30, 60, 120, 240 min. A significant reduction in resistance (50%) is observed for up to 4 h. Blood pressure is monitored; no significant change indicates low systemic absorption.
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| ADME/Pharmacokinetics |
PK of tuaminoheptane after intranasal administration: The compound is rapidly absorbed through the nasal mucosa. Peak plasma concentration (Cmax) is low (typically <10 ng/mL) due to small dose (0.5 mg) and local action. Elimination half-life from plasma is approximately 2-3 h. It is metabolized by amine oxidases and CYP450 to inactive metabolites. Oral bioavailability is high (80%), but the drug is not used orally. Volume of distribution ~2 L/kg. Protein binding ~30%.
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| Toxicity/Toxicokinetics |
Toxicity: At recommended intranasal doses, tuaminoheptane is well-tolerated. Overuse can cause rebound congestion (rhinitis medicamentosa), local irritation, and rarely systemic effects such as hypertension, palpitations, or CNS stimulation. Oral LD50 in rats is ~500 mg/kg. The sulfate salt is not a mutagen. Contraindicated in patients with severe hypertension, coronary artery disease, and hyperthyroidism. Not for prolonged use.
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| References | |
| Additional Infomation |
Tuaminoheptane sulfate (CAS: 6411-75-2) is marketed under brand names such as Tuamine, Rhinaspray, and in combination products. It is an old sympathomimetic amine, first introduced in the 1940s. The chemical structure is heptan-2-amine. It is one of the few volatile amines used in nasal inhalers. Unlike imidazoline decongestants (e.g., oxymetazoline), tuaminoheptane has a shorter duration of action (4-6 hours vs. 8-12 hours) but less risk of rebound congestion. It is available over-the-counter in many countries as an inhaler (0.15-0.5 mg per dose). The sulfate salt is a white crystalline solid, soluble in water. It is also used in veterinary medicine. Due to its sympathomimetic activity, it is on the World Anti-Doping Agency (WADA) prohibited list for in-competition use. The compound is not a controlled substance but requires medical supervision in some jurisdictions. Purity >99%.
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| Molecular Formula |
C7H19NO4S
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|---|---|
| Molecular Weight |
213.30
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| Exact Mass |
328.24
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| CAS # |
6411-75-2
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| Related CAS # |
123-82-0 (Parent)
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| PubChem CID |
44134533
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
21
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| Complexity |
125
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCC(C)N.CCCCCC(C)N.OS(=O)(=O)O
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| InChi Key |
XKUUMWKWUZRRPD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/2C7H17N.H2O4S/c2*1-3-4-5-6-7(2)8;1-5(2,3)4/h2*7H,3-6,8H2,1-2H3;(H2,1,2,3,4)
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| Chemical Name |
bis(heptan-2-amine);sulfuric acid
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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 | 4.6882 mL | 23.4412 mL | 46.8823 mL | |
| 5 mM | 0.9376 mL | 4.6882 mL | 9.3765 mL | |
| 10 mM | 0.4688 mL | 2.3441 mL | 4.6882 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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