Almorexant hydrochloride (Synonyms: ACT 078573 hydrochloride)

Name: Almorexant hydrochloride
Brand: MedChemExpress
SKU: HY-10805A
Rating: 5.0 (5 reviews)

Cat. No.: HY-10805A Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Almorexant (ACT 078573) hydrochloride 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 hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca²⁺ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

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Almorexant hydrochloride Chemical Structure

CAS No. : 913358-93-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 134	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 134	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 111	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 178	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 416	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 666	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1000	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Almorexant hydrochloride:

Almorexant In-stock

4 Publications Citing Use of MCE Almorexant hydrochloride

: Almorexant hydrochloride 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

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•Related Screening Libraries:

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View All Orexin Receptor (OX Receptor) Isoform Specific Products:

View All Isoforms

OX₂ Receptor OX₁ Receptor

View All Calcium Channel Isoform Specific Products:

View All Isoforms

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

View All Caspase Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

human OX2R

0.17 nM (Kd)

human OX1R

1.3 nM (Kd)

Caspase-3

In Vitro

Almorexant hydrochloride (1 μM) promote tyrosine phosphorylation of SHP2/OX1R complex^[1].
Almorexant hydrochloride (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 hydrochloride (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors^[2].
Almorexant hydrochloride (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning^[4].
Almorexant hydrochloride (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy 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.

Clinical Trial

Molecular Weight

549.02

Formula

C₂₉H₃₂ClF₃N₂O₃

CAS No.

913358-93-7

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.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 46 mg/mL (83.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8214 mL	9.1071 mL	18.2143 mL
5 mM	0.3643 mL	1.8214 mL	3.6429 mL
10 mM	0.1821 mL	0.9107 mL	1.8214 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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 (4.55 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.55 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 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.55 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
(per animal)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (286 KB) SDS (252 KB)

COA (260 KB) HNMR (288 KB) LCMS (258 KB)

Handling Instructions (2659 KB)

References

[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	1.8214 mL	9.1071 mL	18.2143 mL	45.5357 mL
	5 mM	0.3643 mL	1.8214 mL	3.6429 mL	9.1071 mL
	10 mM	0.1821 mL	0.9107 mL	1.8214 mL	4.5536 mL
	15 mM	0.1214 mL	0.6071 mL	1.2143 mL	3.0357 mL
	20 mM	0.0911 mL	0.4554 mL	0.9107 mL	2.2768 mL
	25 mM	0.0729 mL	0.3643 mL	0.7286 mL	1.8214 mL
	30 mM	0.0607 mL	0.3036 mL	0.6071 mL	1.5179 mL
	40 mM	0.0455 mL	0.2277 mL	0.4554 mL	1.1384 mL
	50 mM	0.0364 mL	0.1821 mL	0.3643 mL	0.9107 mL
	60 mM	0.0304 mL	0.1518 mL	0.3036 mL	0.7589 mL
	80 mM	0.0228 mL	0.1138 mL	0.2277 mL	0.5692 mL

Almorexant hydrochloride 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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Almorexant hydrochloride (Synonyms: ACT 078573 hydrochloride)

Customer Review

Other Forms of Almorexant hydrochloride:

Almorexant hydrochloride Related Antibodies

4 Publications Citing Use of MCE Almorexant hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Orexin Receptor (OX Receptor) Isoform Specific Products:

View All Calcium Channel Isoform Specific Products:

View All Caspase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Almorexant hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Almorexant hydrochloride Related Classifications

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