Vornorexant (Synonyms: ORN-0829; TS-142)

Name: Vornorexant
Brand: MedChemExpress
SKU: HY-139559
Rating: 4.5 (0 reviews)

Art. -Nr.: HY-139559 Reinheit: 98.41% ee.: 100%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Vornorexant Chemische Struktur

CAS. Nr. : 1517965-94-4

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
1 mg	Auf Lager	Estimated Time of Arrival: December 31
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
200 mg	Angebot einholen
500 mg	Angebot einholen

or Massenanfrage

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

This product is a controlled substance and not for sale in your territory.

Kundenbewertung

Based on 1 Customer Validation

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

OX₂ Receptor OX₁ Receptor

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target

OX₂ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	1.05 1 Compound: (-)-3h, ORN0829	Antagonist activity at human recombinant OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo4-AM dye based fluorescence analysis Antagonist activity at human recombinant OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo4-AM dye based fluorescence analysis	[PMID: 32482533]
CHO-K1	IC₅₀	1.05 1 Compound: (-)-3h, ORN0829	Antagonist activity at human recombinant OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo4-AM dye based fluorescence analysis Antagonist activity at human recombinant OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo4-AM dye based fluorescence analysis	[PMID: 32482533]
CHO-K1	IC₅₀	1.05 1 Compound: (-)-3h, ORN0829	Antagonist activity at human recombinant OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo4-AM dye based fluorescence analysis Antagonist activity at human recombinant OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo4-AM dye based fluorescence analysis	[PMID: 32482533]
CHO-K1	IC₅₀	1.27 1 Compound: (-)-3h, ORN0829	Antagonist activity at human recombinant OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo-4AM dye based fluorescence analysis Antagonist activity at human recombinant OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo-4AM dye based fluorescence analysis	[PMID: 32482533]
CHO-K1	IC₅₀	1.27 1 Compound: (-)-3h, ORN0829	Antagonist activity at human recombinant OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo-4AM dye based fluorescence analysis Antagonist activity at human recombinant OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo-4AM dye based fluorescence analysis	[PMID: 32482533]
CHO-K1	IC₅₀	1.27 1 Compound: (-)-3h, ORN0829	Antagonist activity at human recombinant OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo-4AM dye based fluorescence analysis Antagonist activity at human recombinant OX2R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 30 mins followed by orexin-A stimulation by Fluo-4AM dye based fluorescence analysis	[PMID: 32482533]

In Vivo

Vornorexant (oral administration; 1-10 mg/kg) exhibits potent sleep-promoting effects at a po. dose of 1 mg/kg in a rat polysomnogram study. It results in a dose-dependent increase in the percentage of total sleep^[1].
Vornorexant exhibits optimal PK properties with a rapid T_max and short half-lives in rats and dogs. The T_1/2 is 0.238 hours and 1.16 hours, respectively in rat and dog^[1].

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

Animal Model:	Rat^[1]
Dosage:	1, 3, 10 mg/kg
Administration:	Oral administration to rats prior to turning the light off (start of the active phase); 1-10 mg/kg
Result:	Possessed promising sleep-inducing and sleep-promoting effects.

Klinische Studie

Molekulargewicht

447.46

Formel

C₂₃H₂₂FN₇O₂

CAS. Nr.

1517965-94-4

Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1[C@@H](OCCC1)CN2N=C(C3=CC=C(C=N3)F)C=C2)C4=C(N5N=CC=N5)C=CC(C)=C4

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (223.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2348 mL	11.1742 mL	22.3484 mL
5 mM	0.4470 mL	2.2348 mL	4.4697 mL
10 mM	0.2235 mL	1.1174 mL	2.2348 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner
Verdünnungsrechner

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: ≥ 1.25 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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).

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.

Reinheit & Dokumentation

Purity: 98.41% ee.: 100%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (251 KB) HNMR (275 KB) RP-HPLC (249 KB) LCMS (231 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Aya Futamura, et al. Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia. Bioorg Med Chem. 2020 Jul 1;28(13):115489. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2348 mL	11.1742 mL	22.3484 mL	55.8709 mL
	5 mM	0.4470 mL	2.2348 mL	4.4697 mL	11.1742 mL
	10 mM	0.2235 mL	1.1174 mL	2.2348 mL	5.5871 mL
	15 mM	0.1490 mL	0.7449 mL	1.4899 mL	3.7247 mL
	20 mM	0.1117 mL	0.5587 mL	1.1174 mL	2.7935 mL
	25 mM	0.0894 mL	0.4470 mL	0.8939 mL	2.2348 mL
	30 mM	0.0745 mL	0.3725 mL	0.7449 mL	1.8624 mL
	40 mM	0.0559 mL	0.2794 mL	0.5587 mL	1.3968 mL
	50 mM	0.0447 mL	0.2235 mL	0.4470 mL	1.1174 mL
	60 mM	0.0372 mL	0.1862 mL	0.3725 mL	0.9312 mL
	80 mM	0.0279 mL	0.1397 mL	0.2794 mL	0.6984 mL
	100 mM	0.0223 mL	0.1117 mL	0.2235 mL	0.5587 mL

Vornorexant Related Classifications

Neurological Disease

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.

Keywords:

Vornorexant1517965-94-4ORN-0829 TS-142ORN0829ORN 0829TS142TS 142TS-142Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorinsomniaOX1ROX2Rsleep-promotingInhibitorinhibitorinhibit

Ihre kürzlich angesehenen Produkte:

Produktname

Requested Quantity *

Name des Antragstellers *

Anrede

E-Mail-Addresse *

Telefonnummer *

Department

Name der Organisation *

City

Bundesland

Country or Region *

Bemerkungen

Produktname

Lot #

Name des Antragstellers *

E-Mail-Addresse *

Telefonnummer

Department *

Name der Organisation *

Country or Region *

Bemerkungen

Name
Email *

	Sorry, but the email address you supplied was invalid.

Vornorexant (Synonyms: ORN-0829; TS-142)

Kundenbewertung

Vornorexant Related Antibodies

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Vornorexant Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

Kundenbewertung

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report