1. Cell Cycle/DNA Damage Neuronal Signaling Anti-infection
  2. G-quadruplex Telomerase Cholinesterase (ChE) SARS-CoV
  3. TMPyP4 tosylate

TMPyP4 tosylate  (Synonyms: TMP 1363)

Cat. No.: HY-108477 Purity: ≥98.0%
COA Handling Instructions

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2.

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

TMPyP4 tosylate Chemical Structure

TMPyP4 tosylate Chemical Structure

CAS No. : 36951-72-1

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE TMPyP4 tosylate

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Description

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2[1][2][3][6].

IC50 & Target[2][3][6]

AChE

 

G-quadruplex

 

Telomerase

 

SARS-CoV-2

 

In Vitro

TMPyP4 tosylate (50  µM, 96 h) inhibits telomerase activity in telomerase positive HOS cells[2].
TMPyP4 tosylate (50  µM, 48 or 96 h) inhibits the growth of HOS cells[2].
TMPyP4 tosylate (50  µM, 96 h) induces cell apoptosis in HOS, Saos-2, MG-63, and U2OS cell lines[2].
TMPyP4 tosylate (100  µM, 24 or 48 h) increases cell cycle regulatory proteins and MAPKs in K562 cells[4].

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

Cell Viability Assay[2]

Cell Line: HOS cells
Concentration: 50  µM
Incubation Time: 48 or 96 h
Result: Time-dependently inhibited cell viability.

Western Blot Analysis[4]

Cell Line: K562 cells
Concentration: 100  µM
Incubation Time: 24 or 48 h
Result: Increased the expression of p21CIP1 protein and p57KIP2 protein.
In Vivo

TMPyP4 tosylate (10 and 20 mg/kg, i.p., two times weekly) inhibits tumor growth in MX-1 tumor model[5].
TMPyP4 tosylate (15 mg/kg or 30 mg/kg, i.n.) decreases the mean viral loads in SARS-CoV-2-infected hamster[6].
TMPyP4 tosylate (30 mg/kg, i.n., hamsters) shows a Cmax of 17.88 μg/mL at 1 h, and a half-life (T1/2) of 6.36 h[6].

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

Animal Model: MX-1 mammary chemoadjuvant model[5]
Dosage: 10 and 20 mg/kg
Administration: Intraperitoneal injection (i.p.), twice weekly.
Result: Inhibited tumor growth and prolonged mice survival.
Animal Model: SARS-CoV-2-infected hamster[6]
Dosage: 15 mg/kg or 30 mg/kg
Administration: i.n., starting at 1 h prior to virus inoculation and continuing until 3 days post infection
Result: Decreased the mean viral loads in the nasal wash, nasal turbinate and lung tissues.
Molecular Weight

1363.60

Formula

C72H66N8O12S4

CAS No.
Appearance

Solid

Color

Pale purple to purple

SMILES

C[N+]1=CC=C(/C2=C3C=CC(/C(C4=CC=[N+](C)C=C4)=C5C=C/C(N/5)=C(C6=CC=[N+](C)C=C6)/C(C=C/7)=NC7=C(C8=CC=[N+](C)C=C8)/C9=CC=C2N9)=N\3)C=C1.O=S(C%10=CC=C(C)C=C%10)([O-])=O.O=S(C%11=CC=C(C)C=C%11)([O-])=O.O=S(C%12=CC=C(C)C=C%12)([O-])=O.O=S(C%13=CC=C(C)C=C%13)([O-])=O

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 : 10 mg/mL (7.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (3.67 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7334 mL 3.6668 mL 7.3335 mL
5 mM 0.1467 mL 0.7334 mL 1.4667 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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 1 mg/mL (0.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (0.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

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: 7.14 mg/mL (5.24 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 0.7334 mL 3.6668 mL 7.3335 mL 18.3338 mL
DMSO 5 mM 0.1467 mL 0.7334 mL 1.4667 mL 3.6668 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.

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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.

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