1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. EHT 1864

EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG.

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

EHT 1864 Chemical Structure

EHT 1864 Chemical Structure

CAS No. : 754240-09-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 134 In-stock
Solution
10 mM * 1 mL in DMSO USD 134 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 105 In-stock
10 mg USD 172 In-stock
50 mg USD 602 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

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Based on 10 publication(s) in Google Scholar

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Description

EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG[1][2][3][4].

In Vivo

EHT 1864 (oral administration) displays good tolerability, brain penetrance, and no genotoxicity. EHT 1864 (10 and 40 mg/kg/day; daily; 15 days; intraperitoneal injections) lowers brain Aβ 40 by 37% in guinea pigs[1].

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

Molecular Weight

581.48

Formula

C25H29Cl2F3N2O4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC3=CC=NC4=CC(C(F)(F)F)=CC=C34.[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, 1 years; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (171.97 mM)

DMSO : ≥ 32 mg/mL (55.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7197 mL 8.5987 mL 17.1975 mL
5 mM 0.3439 mL 1.7197 mL 3.4395 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, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

* 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
×
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: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 25 mg/mL (42.99 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • Protocol 2

    Add each solvent one by one:  Saline

    Solubility: 25 mg/mL (42.99 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.
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: 99.85%

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, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.7197 mL 8.5987 mL 17.1975 mL 42.9937 mL
5 mM 0.3439 mL 1.7197 mL 3.4395 mL 8.5987 mL
10 mM 0.1720 mL 0.8599 mL 1.7197 mL 4.2994 mL
15 mM 0.1146 mL 0.5732 mL 1.1465 mL 2.8662 mL
20 mM 0.0860 mL 0.4299 mL 0.8599 mL 2.1497 mL
25 mM 0.0688 mL 0.3439 mL 0.6879 mL 1.7197 mL
30 mM 0.0573 mL 0.2866 mL 0.5732 mL 1.4331 mL
40 mM 0.0430 mL 0.2150 mL 0.4299 mL 1.0748 mL
50 mM 0.0344 mL 0.1720 mL 0.3439 mL 0.8599 mL
H2O 60 mM 0.0287 mL 0.1433 mL 0.2866 mL 0.7166 mL
80 mM 0.0215 mL 0.1075 mL 0.2150 mL 0.5374 mL
100 mM 0.0172 mL 0.0860 mL 0.1720 mL 0.4299 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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EHT 1864 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.

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EHT 1864
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