2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. Vornorexant

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

製品番号: HY-139559 純度: 98.41% ee.: 100%
COA 取扱説明書 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.

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Vornorexant

Vornorexant 構造式

CAS 番号 : 1517965-94-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 440 在庫あり
Solution
10 mM * 1 mL in DMSO USD 440 在庫あり
Solid
1 mg $160 在庫あり
5 mg $400 在庫あり
10 mg $638 在庫あり
25 mg $1275 在庫あり
50 mg $2040 在庫あり
100 mg $3300 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Vornorexant 関連抗体

Top Publications Citing Use of Products

Orexin Receptor (OX Receptor) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
OX2 Receptor OX1 Receptor

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  • 純度とドキュメンテーション

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製品説明

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.

IC50 & Target

OX2 Receptor

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
1.05 nM
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 nM
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]
体内実験

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 Tmax and short half-lives in rats and dogs. The T1/2 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.
臨床実験
分子量

447.46

分子式

C23H22FN7O2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
純度とドキュメンテーション

純度: 98.41% ee.: 100%

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

取扱説明書 (2659 KB)
参考文献

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.

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
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Vornorexant Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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

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