Almorexant (Synonyms: ACT 078573)

Name: Almorexant
Brand: MedChemExpress
SKU: HY-10805
Rating: 5.0 (9 reviews)

Cat. No.: HY-10805 Pureza: 99.96%: Ficha de datos
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Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with K_d values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca²⁺ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

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No. CAS : 871224-64-5

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 9 publication(s) in Google Scholar

Other Forms of Almorexant:

Almorexant hydrochloride In-stock
Almorexant-¹³C,d₃ Obtener un presupuesto
Almorexant (Standard) Obtener un presupuesto

9 Publications Citing Use of MCE Almorexant

: Almorexant purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jan 9;9(6):6952-6967. [Abstract]; Orexin-A and Almorexant promote tyrosine phosphorylation of SHP2/OX1R complex

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Orexin Receptor (OX Receptor):

Ver todas las isoformas

OX₂ Receptor OX₁ Receptor

Ver todos los productos específicos de isoformas Calcium Channel:

Ver todas las isoformas

N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Ver todos los productos específicos de isoformas Caspase:

Ver todas las isoformas

Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

human OX2R

0.17 nM (Kd)

human OX1R

1.3 nM (Kd)

Caspase-3

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	8 1 Compound: ACT-078573	Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	[PMID: 23719231]
CHO	IC₅₀	13 1 Compound: ACT-078573	Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	[PMID: 23719231]
CHO	IC₅₀	13 1 Compound: 15	Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release	[PMID: 26317591]
CHO	IC₅₀	8 1 Compound: 15	Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release	[PMID: 26317591]
CHO	IC₅₀	13 1 Compound: ACT-078573	Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	[PMID: 23719231]
CHO	IC₅₀	8 1 Compound: ACT-078573	Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	[PMID: 23719231]
CHO	IC₅₀	8 1 Compound: 15	Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release	[PMID: 26317591]
CHO	IC₅₀	13 1 Compound: ACT-078573	Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	[PMID: 23719231]
CHO	IC₅₀	13 1 Compound: 15	Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release	[PMID: 26317591]
CHO	IC₅₀	8 1 Compound: ACT-078573	Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	[PMID: 23719231]

In Vitro

Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex^[1].
Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells^[1].

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

In Vivo

Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors^[2].
Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning^[4].
Almorexant (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance^[3].

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

Animal Model:	Mice xenografted with AsPC-1 cells^[2]
Dosage:	1.8 μmol/kg, 100 μL
Administration:	IP, daily, starting at day 0 or day 38
Result:	Resulted in a significant decrease in tumor volume when treatment starting at day 0. Started after AsPC-1 tumors were developed (day 38), rapidly and strongly reduced the volume of established tumors.

Animal Model:	Long-Evans rats (24, male, 16-18 weeks of age)^[4]
Dosage:	300 mg/kg
Administration:	PO, once
Result:	Successfully learned the spatial task, established spatial memory.

Animal Model:	Male C57BL/6 mice (Orexin/ataxin-3 transgenic (TG) mice and WT mice, 32 ± 0.9 g, age 15 ± 0.5 week)^[3]
Dosage:	30, 100, 300 mg/kg (3, 10, and 30 mg/mL; 10 mL/kg)
Administration:	IP, once every 3 days
Result:	Exacerbated cataplexy in TG mice and increased nonrapid eye movement (NREM) sleep with heightened sleep/wake fragmentation in both genotypes during the 12-h dark period after dosing. Showed greater hypnotic potency in WT mice than in TG mice.

Peso molecular

512.56

Fòrmula

C₂₉H₃₁F₃N₂O₃

No. CAS

871224-64-5

Appearance

Solid

Color

White to off-white

SMILES

CNC([C@@H](C1=CC=CC=C1)N2CCC3=CC(OC)=C(OC)C=C3[C@@H]2CCC4=CC=C(C(F)(F)F)C=C4)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (195.10 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	1.9510 mL	9.7550 mL	19.5099 mL
5 mM	0.3902 mL	1.9510 mL	3.9020 mL
10 mM	0.1951 mL	0.9755 mL	1.9510 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.

Calculadora de molaridad
Calculadora de dilución

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (4.88 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 (4.88 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
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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.

Pureza y Documentación

Purity: 99.96%

Select Batch:

Ficha de datos (283 KB) SDS (252 KB)

COA (255 KB) HNMR (454 KB) RP-HPLC (244 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Dayot S, et al. In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma. Oncotarget. 2018 Jan 9;9(6):6952-6967. [Content Brief]

[2]. Malherbe P, et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31. [Content Brief]

[3]. Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36(3):325-36. [Content Brief]

[4]. Dietrich H, et al. Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl). 2010 Oct;212(2):145-54. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9510 mL	9.7550 mL	19.5099 mL	48.7748 mL
	5 mM	0.3902 mL	1.9510 mL	3.9020 mL	9.7550 mL
	10 mM	0.1951 mL	0.9755 mL	1.9510 mL	4.8775 mL
	15 mM	0.1301 mL	0.6503 mL	1.3007 mL	3.2517 mL
	20 mM	0.0975 mL	0.4877 mL	0.9755 mL	2.4387 mL
	25 mM	0.0780 mL	0.3902 mL	0.7804 mL	1.9510 mL
	30 mM	0.0650 mL	0.3252 mL	0.6503 mL	1.6258 mL
	40 mM	0.0488 mL	0.2439 mL	0.4877 mL	1.2194 mL
	50 mM	0.0390 mL	0.1951 mL	0.3902 mL	0.9755 mL
	60 mM	0.0325 mL	0.1626 mL	0.3252 mL	0.8129 mL
	80 mM	0.0244 mL	0.1219 mL	0.2439 mL	0.6097 mL
	100 mM	0.0195 mL	0.0975 mL	0.1951 mL	0.4877 mL

Almorexant Related Classifications

Help & FAQs

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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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Almorexant (Synonyms: ACT 078573)

Revisión del cliente

Other Forms of Almorexant:

Almorexant Related Antibodies

9 Publications Citing Use of MCE Almorexant

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Orexin Receptor (OX Receptor):

Ver todos los productos específicos de isoformas Calcium Channel:

Ver todos los productos específicos de isoformas Caspase:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Almorexant Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Almorexant Related Classifications

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Productos vistos recientemente:

Revisión del cliente

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