Philanthotoxin 74 dihydrochloride (Synonyms: PhTx 74 dihydrochloride)

Name: Philanthotoxin 74 dihydrochloride
Brand: MedChemExpress
SKU: HY-104020A
Rating: 4.5 (1 reviews)

Cat. No.: HY-104020A Purity: 98.47%: FAQs
Data Sheet SDS COA Handling Instructions

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Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC₅₀s of 263 and 296 nM, respectively.

For research use only. We do not sell to patients.

Philanthotoxin 74 dihydrochloride Chemical Structure

CAS No. : 1227301-51-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 118	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 118	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC₅₀s of 263 and 296 nM, respectively.

IC₅₀ & Target

IC50: 296 nM (GluR1), 296 nM (GluR1)^[1]

Ki: 0.29 μM (GluR5Q)^[2]

In Vitro

Philanthotoxin 74 in the micromolar concentration range displays selective inhibition between the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 is reported to fully inhibit GluA1/A2R receptors when applied at a concentration of 500 μM while producing 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74, when tested at concentrations of 100 and 500 μM, displays pronounced channel block (more than 80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Oocytes expressing GluA2R alone that homomeric GluA2R is virtually inert to philanthotoxin 74 in the 0.1-300 μM concentration range, displaying less than 5% inhibition at the maximum tested concentration of 300 μM. Philanthotoxin 74 inhibits these receptors nonselectively, with IC₅₀ values of about 30 μM, in both the presence and absence of γ-2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

507.54

Formula

C₂₄H₄₄Cl₂N₄O₃

CAS No.

1227301-51-0

Appearance

Solid

Color

White to light yellow

SMILES

O=C(NCCCCCCCNCCCCN)[C@@H](NC(CCC)=O)CC1=CC=C(O)C=C1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (197.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (98.51 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9703 mL	9.8514 mL	19.7029 mL
5 mM	0.3941 mL	1.9703 mL	3.9406 mL
10 mM	0.1970 mL	0.9851 mL	1.9703 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (98.51 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.47%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (243 KB) HNMR (275 KB) LCMS (257 KB)

Handling Instructions (2659 KB)

References

[1]. Poulsen MH, et al. Evaluation of PhTX-74 as subtype-selective inhibitor of GluA2-containing AMPA receptors. Mol Pharmacol. 2014 Feb;85(2):261-8. [Content Brief]

[2]. Kromann H, et al. Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors. J Med Chem. 2002 Dec 19;45(26):5745-54. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.9703 mL	9.8514 mL	19.7029 mL	49.2572 mL
	5 mM	0.3941 mL	1.9703 mL	3.9406 mL	9.8514 mL
	10 mM	0.1970 mL	0.9851 mL	1.9703 mL	4.9257 mL
	15 mM	0.1314 mL	0.6568 mL	1.3135 mL	3.2838 mL
	20 mM	0.0985 mL	0.4926 mL	0.9851 mL	2.4629 mL
	25 mM	0.0788 mL	0.3941 mL	0.7881 mL	1.9703 mL
	30 mM	0.0657 mL	0.3284 mL	0.6568 mL	1.6419 mL
	40 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2314 mL
	50 mM	0.0394 mL	0.1970 mL	0.3941 mL	0.9851 mL
	60 mM	0.0328 mL	0.1642 mL	0.3284 mL	0.8210 mL
	80 mM	0.0246 mL	0.1231 mL	0.2463 mL	0.6157 mL
DMSO	100 mM	0.0197 mL	0.0985 mL	0.1970 mL	0.4926 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Philanthotoxin 74 dihydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Philanthotoxin 741227301-51-0PhTx 74Philanthotoxin74Philanthotoxin-74PhTx74PhTx-74iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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Philanthotoxin 74 dihydrochloride (Synonyms: PhTx 74 dihydrochloride)

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Philanthotoxin 74 dihydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Philanthotoxin 74 dihydrochloride Related Classifications

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