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EST64454 hydrochloride (Synonyms: EST64454 HCL)

Name: EST64454 hydrochloride
Brand: TargetMol
SKU: T8834
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T8834 Copy Product Info

Purity: 99.28%

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EST64454 hydrochloride (EST64454) is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.

EST64454 hydrochloride

Copy Product Info

🥰Excellent

Catalog No. T8834

Synonyms EST64454 HCL

EST64454 hydrochloride (EST64454) is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.

Cas No. 1950569-11-5

Pack Size	Price	USA Stock	Global Stock
1 mg	$30	-	In Stock
5 mg	$59	-	In Stock
10 mg	$98	-	In Stock
25 mg	$208	-	In Stock
50 mg	$337	-	In Stock
100 mg	$535	-	In Stock
1 mL x 10 mM (in DMSO)	$74	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.28%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

EST64454 hydrochloride AI Summary

EST64454 hydrochloride shows high affinity for the sigma1 receptor with a Ki value of 22.0 nM, indicating antagonist activity. It demonstrates analgesic activity in mouse models of mechanical hypersensitivity-induced pain and maintains good oral bioavailability in both CD1 mice and Wistar rats. However, it has low solubility but moderate permeability. In liver microsome assays, the compound exhibited potent inhibition of various CYP enzymes, although it showed low affinity for the sigma2 receptor. Additionally, EST64454 hydrochloride has a relatively short elimination half-life and a high volume of distribution at steady state in both species tested..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	EST64454 hydrochloride (EST64454) is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.
Targets&IC50	σ1 receptor:22 nM(Ki)
Synonyms	EST64454 HCL

Chemical Properties

Molecular Weight	400.85
Formula	C₁₈H₂₃ClF₂N₄O₂
Cas No.	1950569-11-5
Smiles	Cl.CC(=O)N1CCN(CCOCc2ccn(n2)-c2ccc(F)c(F)c2)CC1
Relative Density.	no data available

Storage & Solubility Information

Storage

Store at low temperature | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 20 mg/mL (49.89 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.99 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4947 mL	12.4735 mL	24.9470 mL	124.7349 mL
5 mM	0.4989 mL	2.4947 mL	4.9894 mL	24.9470 mL
10 mM	0.2495 mL	1.2473 mL	2.4947 mL	12.4735 mL
20 mM	0.1247 mL	0.6237 mL	1.2473 mL	6.2367 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc