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HsTX1 TFA

Cat No.:V84003 Purity: ≥98%
HsTX1 TFA
HsTX1 TFA Chemical Structure Product category: Potassium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes
Official Supplier of:
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Product Description
HsTX1 (TFA) toxin is derived from the scorpion Heterometrus spinnifer and is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is a potassium channel inhibitor with an IC50 value of 12 pM for Kv1.3, which can inhibit TEM cell activation and reduce autoimmune inflammation.
HsTX1 TFA is a toxin derived from the scorpion Heterometrus spinnifer. It is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is a potent potassium channel inhibitor with an IC50 of 12 pM for Kv1.3. It inhibits TEM cell activation and attenuates inflammation in autoimmunity. It is intended for research use only.
Biological Activity I Assay Protocols (From Reference)
Targets
HsTX1 TFA targets the potassium channel Kv1.3, a voltage-gated potassium channel that plays a critical role in T cell activation and immune regulation. It inhibits Kv1.3 with an IC50 of 12 pM. By blocking Kv1.3, HsTX1 inhibits TEM (effector memory T) cell activation and attenuates inflammation in autoimmune conditions. The peptide's four disulfide bridges confer structural stability.
ln Vitro
In vitro studies demonstrate that HsTX1 TFA is a potent inhibitor of the potassium channel Kv1.3 with an IC50 of 12 pM. This picomolar potency indicates extremely high affinity for the channel. By inhibiting Kv1.3, the compound inhibits TEM cell activation. The peptide is derived from the scorpion Heterometrus spinnifer and consists of 34 residues with four disulfide bridges.
ln Vivo
In vivo activity of HsTX1 TFA is inferred from its mechanism as a Kv1.3 inhibitor that attenuates inflammation in autoimmunity. By inhibiting TEM cell activation, the peptide may reduce autoimmune inflammatory responses. Detailed in vivo efficacy data from animal models of autoimmune disease are not extensively documented in the available literature. The compound is intended for research use only.
Enzyme Assay
The in vitro enzyme/receptor binding assay for HsTX1 TFA involves measuring its inhibitory activity against the Kv1.3 potassium channel. Patch-clamp electrophysiology is the standard method for assessing potassium channel inhibition. Cells expressing Kv1.3 are treated with the peptide at varying concentrations, and potassium currents are measured. IC50 values are determined from dose-response curves. Standard protocols include appropriate positive controls such as known Kv1.3 inhibitors.
Cell Assay
In vitro cell-based assays for HsTX1 TFA are conducted using T cells to evaluate its effects on cell activation. Cells are treated with the peptide at various concentrations, and T cell activation is assessed by measuring cytokine production, proliferation, and surface marker expression. TEM cell activation is specifically evaluated. Cytotoxicity is evaluated using standard cell viability assays.
Animal Protocol
In vivo animal studies for HsTX1 TFA would typically be conducted using mouse models of autoimmune disease. Animals would be administered the peptide via appropriate routes, and inflammation would be assessed by measuring inflammatory markers, cytokine levels, and histopathological changes. TEM cell activation in tissues would be evaluated. However, detailed in vivo protocols and efficacy data are not available from the search results.
ADME/Pharmacokinetics
Pharmacokinetic properties of HsTX1 TFA include its nature as a 34-residue peptide with four disulfide bridges. As a peptide toxin, it is subject to proteolytic degradation and may have limited oral bioavailability. The TFA salt form is used to enhance solubility and stability. Detailed pharmacokinetic parameters are not extensively documented in the available literature.
Toxicity/Toxicokinetics
Toxicity information for HsTX1 TFA is limited. As a peptide toxin derived from scorpion venom, it may have significant toxicity at higher concentrations. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
References

[1].A potent and Kv1.3-selective analogue of the scorpion toxin HsTX1 as a potential therapeutic for autoimmune diseases. Sci Rep. 2014 Mar 28:4:4509. doi: 10.1038/srep04509.

[2].A four-disulphide-bridged toxin, with high affinity towards voltage-gated K+ channels, isolated from Heterometrus spinnifer (Scorpionidae) venom. Biochemical Journal. 328 (Pt 1): 321–327.

[3].Prolonged immunomodulation in inflammatory arthritis using the selective Kv1.3 channel blocker HsTX1[R14A] and its PEGylated analog. Immunol. 2017 Jul; 180: 45–57. Published online 2017 Apr 4.

Additional Infomation
HsTX1 TFA is a peptide toxin from the scorpion Heterometrus spinnifer that inhibits the potassium channel Kv1.3 with an IC50 of 12 pM. It is a 34-residue, C-terminally amidated peptide with four disulfide bridges. It inhibits TEM cell activation and attenuates autoimmune inflammation. It is intended for research use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C149H246N54O46S9.XC2HF3O2
Molecular Weight
3818.47 (free base)
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)
H2O :~50 mg/mL (with sonication)
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.)
Calculator

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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?
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  • 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:
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  • 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)
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  • 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:
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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)
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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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