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Almorexant hydrochloride

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Catalog No. T6155Cas No. 913358-93-7
Alias Orexin-RA-1 hydrochloride, ACT-078573 hydrochloride, ACT 078573 hydrochloride, A 573 hydrochloride

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

Almorexant hydrochloride

Almorexant hydrochloride

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Purity: 99.85%
Catalog No. T6155Alias Orexin-RA-1 hydrochloride, ACT-078573 hydrochloride, ACT 078573 hydrochloride, A 573 hydrochlorideCas No. 913358-93-7
Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$35-In Stock
5 mg$90-In Stock
10 mg$146-In Stock
25 mg$343-In Stock
50 mg$549-In Stock
100 mg$828-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.85%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.
Targets&IC50
OX1:1.3 nM(ki), OX2:0.17 nM(ki)
In vitro
AsPC-1 cells preincubated or not with the SHP2 inhibitor NSC-87877 (50 μM) were challenged for 5 min without or with 1 μM orexin-A or 1 μM Almorexant hydrochloride. In parallel, HPAF-II cells were also challenged for 5 min without or with 1 μM orexin-A. Orexin-A and Almorexant hydrochloride promote tyrosine phosphorylation of SHP2/OX1R complex. [1]
In vivo
Daily intraperitoneal injection of Almorexant hydrochloride (1.8 μmol/kg) at day 0 in mice xenografted with AsPC-1 cells and up to the mice sacrifices resulted in a significant decrease in tumor volume (> 50%), as compared to untreated mice. Treatment with Almorexant hydrochloride started after AsPC-1 tumors were developed, rapidly and strongly reduced the volume of established tumors. OX1R expression revealed by immunodetection was not affected by Almorexant hydrochloride treatment. [1]
SynonymsOrexin-RA-1 hydrochloride, ACT-078573 hydrochloride, ACT 078573 hydrochloride, A 573 hydrochloride
Chemical Properties
Molecular Weight549.02
FormulaC29H32ClF3N2O3
Cas No.913358-93-7
SmilesC(CC1=CC=C(C(F)(F)F)C=C1)[C@H]2C=3C(=CC(OC)=C(OC)C3)CCN2[C@@H](C(NC)=O)C4=CC=CC=C4.Cl
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 48 mg/mL (87.43 mM), Sonication is recommended.
DMSO: 40 mg/mL (72.86 mM), Sonication is recommended.
H2O: < 0.1 mg/mL (insoluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.64 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/Ethanol
1mg5mg10mg50mg
1 mM1.8214 mL9.1071 mL18.2143 mL91.0714 mL
5 mM0.3643 mL1.8214 mL3.6429 mL18.2143 mL
10 mM0.1821 mL0.9107 mL1.8214 mL9.1071 mL
20 mM0.0911 mL0.4554 mL0.9107 mL4.5536 mL
50 mM0.0364 mL0.1821 mL0.3643 mL1.8214 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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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

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