| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Claramine TFA targets the lipid bilayer of cell membranes. It is a steroidal polyamine that modulates membrane properties, affecting membrane fluidity, curvature, and permeability. By stabilizing the membrane, Claramine TFA protects cells from the toxic effects of various biological toxins, including misfolded protein oligomers (e.g., alpha-synuclein oligomers, amyloid-beta oligomers) and other protein-derived toxins. It does not have a specific receptor target but acts on the membrane to prevent toxin insertion and pore formation. This mechanism of action is distinct from conventional receptor antagonists.
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| ln Vitro |
Claramine (2-20 μM; 20 h) does not affect cell viability in human neuroblastoma (SH-SY5Y) cells at concentrations below 10 μM. Claramine (2-20 μM; 20 h) does not affect cell viability in HEK293 cells[1]. Claramine (2.5-10 μM; 20 h) protects human neuroblastoma (SH-SY5Y) cells from the pore-forming agents melittin (4 μM; 20 h) and α-hemolysin (50 μg/mL; 20 h) by inhibiting their binding to the cell membrane[1].
In vitro, Claramine TFA (2.5-10 microM, 20 h) protects human neuroblastoma SH-SY5Y cells from the toxicity of misfolded protein oligomers. It regulates the properties of lipid membranes and protects cells from various biological toxins. The compound is a steroidal polyamine. It can be used to study the cellular mechanisms underlying protein misfolding diseases such as Alzheimer‘s disease, Parkinson's disease, and Huntington‘s disease. Specific IC₅0 values are not provided. |
| ln Vivo |
In vivo, Claramine TFA can be used to study neuroprotection in animal models of protein misfolding diseases. By stabilizing cell membranes and blocking the toxic effects of protein oligomers, it may reduce neurodegeneration and improve behavioral outcomes. No specific in vivo efficacy data is detailed. The compound is a research-grade chemical, not an approved drug. It is being investigated as a potential therapeutic for prion diseases and other neurodegenerative disorders.
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| Enzyme Assay |
The membrane-stabilizing activity of Claramine TFA can be assessed using liposome leakage assays. Liposomes (large unilamellar vesicles) are prepared from phospholipids (e.g., POPC or brain lipid extract) and loaded with a fluorescent dye (e.g., calcein at self-quenching concentration). Toxin (e.g., alpha-synuclein oligomers or melittin) is added, causing membrane disruption and dye release (increase in fluorescence). Claramine TFA (0.1-100 uM) is pre-incubated with the liposomes or added before the toxin. The protection of membrane integrity is measured by the reduction in fluorescence. The EC50 for protection is calculated.
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| Cell Assay |
For cell-based assays, SH-SY5Y cells are seeded in 96-well plates (1×10⁴ cells/well) and differentiated with retinoic acid (10 uM) for 5-7 days. Cells are pre-treated with Claramine TFA (1-50 uM) for 1 h, then exposed to misfolded protein oligomers (e.g., alpha-synuclein oligomers, 1-10 uM) or other toxins for 24-48 h. Cell viability is measured by MTT assay. The protection (EC50) is calculated. Calcium influx is measured by Fluo-4 AM fluorescence. Reactive oxygen species (ROS) are measured by DCFH-DA. Membrane integrity is assessed by LDH release.
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| Animal Protocol |
In vivo efficacy can be evaluated in a mouse model of Parkinson‘s disease (e.g., alpha-synuclein pre-formed fibril injection model). Male C57BL/6 mice (6-8 wk, n=10/group) are injected stereotaxically with alpha-synuclein pre-formed fibrils (PFFs) into the striatum to induce synucleinopathy. Claramine TFA is formulated in 10% DMSO + 5% Tween 80 + 85% saline and administered intraperitoneally (IP) at doses of 10-50 mg/kg once daily for 4-8 weeks. Motor function is assessed by rotarod and open field tests. Brain tissues are harvested for immunohistochemistry (alpha-synuclein, tyrosine hydroxylase) and measurement of neuroinflammation (Iba-1, GFAP). No specific data is available.
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| ADME/Pharmacokinetics |
No specific PK data for Claramine TFA is available. As a steroidal polyamine (MW 703.02), it has limited oral bioavailability. It is likely injected IP or IV for in vivo studies. The TFA salt form improves solubility. The compound is expected to have a half-life of 2-6 hours in rodents. For research use, it is stored as a powder at -20degC (powder: -20degC for 3 years, 4degC for 2 years; in solvent: -80degC for 6 months, -20degC for 1 month) under nitrogen, protected from light.
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| Toxicity/Toxicokinetics |
For Claramine TFA, hazard statements: H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation). Signal word: Warning. Precautionary statements: P261 (Avoid breathing dust/fume/gas/mist/vapors/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes). Storage: at -20degC, under nitrogen, sealed, protect from light.
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| References | |
| Additional Infomation |
Claramine TFA (CAS# 3030428-57-7) is a research-grade steroidal polyamine and membrane-stabilizing agent. It is not an FDA-approved drug. It is used to study protein misfolding disorders (neurodegenerative diseases) and to protect cells from various biological toxins. For research use only, not for diagnostic or therapeutic applications. Purity: ≥98%. Storage: -20degC, sealed, protect from light.
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| Molecular Formula |
C39H73F3N4O3
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| Molecular Weight |
703.02
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| Exact Mass |
702.563
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| CAS # |
3030428-57-7
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| Related CAS # |
Claramine;1430194-56-1
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| PubChem CID |
171364513
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
49
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| Complexity |
860
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@H](CCCC(C)C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2C[C@H](C4[C@@]3(CC[C@@H](C4)O)C)NCCCNCCCCNCCCN)C.C(=O)(C(F)(F)F)O
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| InChi Key |
IQNUPEHYBSIFDX-ULTNOTTESA-N
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| InChi Code |
InChI=1S/C37H72N4O.C2HF3O2/c1-27(2)11-8-12-28(3)31-13-14-32-30-26-35(41-24-10-23-40-21-7-6-20-39-22-9-19-38)34-25-29(42)15-17-37(34,5)33(30)16-18-36(31,32)4;3-2(4,5)1(6)7/h27-35,39-42H,6-26,38H2,1-5H3;(H,6,7)/t28-,29+,30+,31-,32+,33+,34?,35-,36-,37-;/m1./s1
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| Chemical Name |
(3S,6R,8S,9S,10R,13R,14S,17R)-6-[3-[4-(3-aminopropylamino)butylamino]propylamino]-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-ol;2,2,2-trifluoroacetic 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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 : ~120 mg/mL (~170.69 mM; with ultrasonication (<60°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (4.27 mM)(saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300, mix well; then add 50 μL Tween-80 to the above system, mix well; then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution. Solubility in Formulation 2: ≥ 3 mg/mL (4.27 mM)(saturation unknown) in 10% DMSO 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one),clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. 2 g SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder is diluted to 10 mL of saline and completely dissolved until clear and transparent. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4224 mL | 7.1122 mL | 14.2243 mL | |
| 5 mM | 0.2845 mL | 1.4224 mL | 2.8449 mL | |
| 10 mM | 0.1422 mL | 0.7112 mL | 1.4224 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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