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  3. EHT 1864

EHT 1864 

Cat. No.: HY-16659 Purity: 99.85%
Handling Instructions

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.

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
Solution
10 mM * 1 mL in DMSO USD 138 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 138 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

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Based on 4 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[1][2][3].

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].

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

Molecular Weight

581.48

Formula

C₂₅H₂₉Cl₂F₃N₂O₄S

CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (171.97 mM)

DMSO : ≥ 32 mg/mL (55.03 mM)

*"≥" 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
10 mM 0.1720 mL 0.8599 mL 1.7197 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.85%

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Keywords:

EHT 1864EHT1864EHT-1864Rasβ-amyloidamyloidprecursorproteinAlzheimerdiseasetransformationInhibitorinhibitorinhibit

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Product Name:
EHT 1864
Cat. No.:
HY-16659
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