2. Neuronal Signaling
  3. Sigma Receptor
  4. Ditolylguanidine

Ditolylguanidine  (Synonyms: 1,3-Di-o-tolylguanidine; DTG)

Cat. No.: HY-14218 Purity: 99.03%
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Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer.

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

Ditolylguanidine Chemical Structure

Ditolylguanidine Chemical Structure

CAS No. : 97-39-2

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Based on 2 publication(s) in Google Scholar

Ditolylguanidine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer[1][2][3][4].

IC50 & Target

Sigma 1 Receptor

 

Sigma 2 Receptor

 

In Vitro

Ditolylguanidine (39-60 nM) dose-dependently inhibits N-(2-piperidinoethyl)4-iodobenzamide) (IPAB) with a Ki value of 40 nM[2].
Ditolylguanidine inhibits small cell lung cancer cells lines NCI-N417 and NCI-H209 with IC50 values of 100 and 90 nM, respectively[3].
Ditolylguanidine (0-10 μM) shows Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively[4].

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

Ditolylguanidine Related Antibodies
In Vivo

Ditolylguanidine (i.v.; 1-5 mg/kg, once) affects micturition intervals and the threshold pressure of anaesthetized rats[1].
Ditolylguanidine (intracerebroventricular administration; 1 μg, once) extends micturition intervals and raises the threshold pressure of anaesthetized rats[1].

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

Animal Model: Urethane anaesthetized male Std-Wistar rats[1]
Dosage: 1-5 mg/kg
Administration: Intravenous injection; 1-5 mg/kg, once
Result: Dose-dependently extended micturition intervals and raised the threshold pressure. Abolished the micturition reflex and urinary dribbling at a dose of 5 mg/kg.
Molecular Weight

239.32

Formula

C15H17N3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(NC(NC2=CC=CC=C2C)=N)C=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (626.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1785 mL 20.8925 mL 41.7851 mL
5 mM 0.8357 mL 4.1785 mL 8.3570 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 2.5 mg/mL (10.45 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.45 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.

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).
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1785 mL 20.8925 mL 41.7851 mL 104.4626 mL
5 mM 0.8357 mL 4.1785 mL 8.3570 mL 20.8925 mL
10 mM 0.4179 mL 2.0893 mL 4.1785 mL 10.4463 mL
15 mM 0.2786 mL 1.3928 mL 2.7857 mL 6.9642 mL
20 mM 0.2089 mL 1.0446 mL 2.0893 mL 5.2231 mL
25 mM 0.1671 mL 0.8357 mL 1.6714 mL 4.1785 mL
30 mM 0.1393 mL 0.6964 mL 1.3928 mL 3.4821 mL
40 mM 0.1045 mL 0.5223 mL 1.0446 mL 2.6116 mL
50 mM 0.0836 mL 0.4179 mL 0.8357 mL 2.0893 mL
60 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7410 mL
80 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
100 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0446 mL
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Ditolylguanidine 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:

Ditolylguanidine97-39-21,3-Di-o-tolylguanidine DTGSigma ReceptorIPABsmall cell lung cancerNCI-N417NCI-H209micturition intervalthreshold pressureratInhibitorinhibitorinhibit

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