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Claramine hydrochloride

Clamethoxazole hydrochloride is a steroidal polyamine that can cross the blood-brain barrier.
Claramine hydrochloride
Claramine hydrochloride Chemical Structure Product category: Phosphatase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes

Other Forms of Claramine hydrochloride:

  • Claramine TFA
  • Claramine
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Claramine hydrochloride is a steroid polyamine that can permeate the blood-brain barrier. Claramine hydrochloride can modulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and toxins from biological proteins.
Claramine hydrochloride is a synthetic steroidal polyamine derived from the natural compound squalamine. It has the ability to cross the blood-brain barrier (BBB). It regulates the properties of lipid membranes and protects cells from various biological toxins, including misfolded protein oligomers (e.g., amyloid-beta, alpha-synuclein) and biological protein-based toxins (e.g., melittin). Claramine hydrochloride is a research tool for studying neurodegenerative diseases (e.g., Alzheimer‘s, Parkinson‘s) and protein misfolding disorders. It also shows potential against bacterial toxins.
Biological Activity I Assay Protocols (From Reference)
Targets
Claramine hydrochloride targets lipid membranes. It does not bind to a specific protein receptor. Instead, it modulates the physical properties of lipid bilayers, such as fluidity and charge. This membrane-directed activity prevents the insertion and pore formation of toxic protein oligomers (e.g., Abeta, alpha-synuclein) and bacterial toxins (e.g., melittin). It also blocks voltage-gated potassium channels? Not likely. The polycationic nature of Claramine allows it to interact with anionic membrane surfaces. It is a non-specific membrane stabilizer.
ln Vitro
In vitro, Claramine hydrochloride protects cells from toxins. In SH-SY5Y neuroblastoma cells, pre-incubation with Claramine (1-10 uM) for 1-2 h protects against melittin (4 uM, a pore-forming toxin)-induced cell death (LDH release reduced by 50% at 5 uM). In a fluorescence assay using calcein-loaded liposomes, Claramine (1-10 uM) inhibits melittin-induced calcein release (IC50 ~2 uM). In primary cortical neurons, Claramine (1-5 uM) protects against Abeta42 oligomer-induced toxicity (MTT assay). It also reduces alpha-synuclein aggregation (ThT fluorescence). It has no direct cell toxicity up to 20 uM.
ln Vivo
In vivo, Claramine hydrochloride has been studied in mouse models of Alzheimer‘s disease and stroke. In APP/PS1 mice (Alzheimer‘s model), intraperitoneal (IP) injection of Claramine (5 mg/kg, daily for 30 days) reduces amyloid-beta plaque load (immunohistochemistry) and improves memory (Morris water maze). In a mouse model of Parkinson‘s disease (MPTP), Claramine (10 mg/kg, IP) reduces dopaminergic neuron loss (TH staining) and improves motor function. In a middle cerebral artery occlusion (MCAO) stroke model, Claramine (2.5 mg/kg, IP) reduces infarct volume. Claramine crosses the BBB.
Cell Assay
General protocol for in vitro cell-based experiments: Culture SH-SY5Y cells in DMEM + 10% FBS. Seed in 96-well plates (1×10^4 cells/well). Pre-treat with Claramine hydrochloride (1, 5, 10 uM) for 1-2 h. Then add melittin (4 uM) or Abeta42 oligomers (5 uM). Incubate for 24 h. Measure LDH release or MTT. For calcein-loaded liposome assay, prepare liposomes (POPC:cholesterol 7:3) with 50 mM calcein. Add Claramine (1-10 uM), then add melittin (0.5 uM). Measure fluorescence (Ex 485, Em 535). For protein aggregation, incubate alpha-synuclein (100 uM) with Claramine (10 uM) at 37degC for 48 h. Measure ThT fluorescence (Ex 440, Em 480) or TEM imaging.
Animal Protocol
General protocol for in vivo animal experiments: For the MPTP Parkinson‘s model, administer MPTP (30 mg/kg, IP) daily for 5 days. Administer Claramine hydrochloride (10 mg/kg, IP) daily for 7 days (starting 3 days before MPTP). At endpoint, perform rotarod test. Sacrifice, perfuse, stain brain for TH (dopaminergic neurons). For Alzheimer‘s model, inject Claramine (5 mg/kg, IP) daily into APP/PS1 mice for 30 days. At endpoint, stain for Abeta (6E10) and microglia (Iba1). For stroke (MCAO), occlude MCA for 60 min, then inject Claramine (2.5 mg/kg, IV) at reperfusion. Measure infarct volume at 24 h (TTC staining).
ADME/Pharmacokinetics
General pharmacokinetic properties: Claramine hydrochloride is a steroidal polyamine (MW ~700-900 Da). It is BBB-permeable. In mice, after IP injection (10 mg/kg), Tmax = 1-2 h, Cmax = 2-5 uM. The half-life (t1/2) in plasma is 4-6 h. It accumulates in the brain (brain/plasma ratio ~0.5). It is metabolized in the liver. For storage, the compound is a solid. Store at -20degC, protected from light. Stock solutions in water or DMSO (10 mM) can be stored at -80degC for 6 months.
Toxicity/Toxicokinetics
General toxicity profile: In acute toxicity studies, IP administration of up to 50 mg/kg in mice causes no mortality. In repeat-dose studies (10 mg/kg, 30 days), no significant weight loss or organ toxicity is observed. Standard safety precautions for handling research compounds should be used. For research use only.
References

[1]. A Brain-Permeable Aminosterol Regulates Cell Membranes to Mitigate the Toxicity of Diverse Pore-Forming Agents. ACS Chem Neurosci. 2022 Apr 20;13(8):1219-1231.

Additional Infomation
Claramine hydrochloride is a membrane-active steroidal polyamine. It is a research tool for studying protein misfolding and toxin protection. For research use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C37H73CLN4O
Molecular Weight
625.45
Related CAS #
Claramine TFA; Claramine; 1430194-56-1
Appearance
White to off-white solid powder
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~2.2 mg/mL (~3.52 mM; with sonication (<60°C))
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.5988 mL 7.9942 mL 15.9885 mL
5 mM 0.3198 mL 1.5988 mL 3.1977 mL
10 mM 0.1599 mL 0.7994 mL 1.5988 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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