2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. ACT-462206

ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research.

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ACT-462206

ACT-462206 構造式

CAS 番号 : 1361321-96-1

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 115 在庫あり
Solution
10 mM * 1 mL in DMSO USD 115 在庫あり
Solid
5 mg $105 在庫あり
10 mg $170 在庫あり
25 mg $357 在庫あり
50 mg $570 在庫あり
100 mg $900 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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Based on 0 publication(s) in Google Scholar

Other Forms of ACT-462206:

ACT-462206 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

ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research[1].

IC50 & Target

OX2

 

OX1

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
11 1
Compound: 22; ACT-462206
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
[PMID: 26317591]
CHO IC50
11 1
Compound: 21, ACT-462206
Antagonist activity at recombinant orexin-2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
Antagonist activity at recombinant orexin-2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
[PMID: 26045032]
CHO IC50
11 1
Compound: 22; ACT-462206
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
[PMID: 26317591]
CHO IC50
11 1
Compound: 21, ACT-462206
Antagonist activity at recombinant orexin-2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
Antagonist activity at recombinant orexin-2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
[PMID: 26045032]
CHO IC50
11 1
Compound: 21, ACT-462206
Antagonist activity at recombinant orexin-2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
Antagonist activity at recombinant orexin-2 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
[PMID: 26045032]
CHO IC50
11 1
Compound: 22; ACT-462206
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
[PMID: 26317591]
CHO IC50
60 1
Compound: 22; ACT-462206
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
[PMID: 26317591]
CHO IC50
60 1
Compound: 22; ACT-462206
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
[PMID: 26317591]
CHO IC50
60 1
Compound: 21, ACT-462206
Antagonist activity at recombinant orexin-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
Antagonist activity at recombinant orexin-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
[PMID: 26045032]
CHO IC50
60 1
Compound: 22; ACT-462206
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release by FLIPR assay
[PMID: 26317591]
CHO IC50
60 1
Compound: 21, ACT-462206
Antagonist activity at recombinant orexin-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
Antagonist activity at recombinant orexin-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
[PMID: 26045032]
CHO IC50
60 1
Compound: 21, ACT-462206
Antagonist activity at recombinant orexin-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
Antagonist activity at recombinant orexin-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of orexin-A-induced Ca2+ flux preincubated for 120 mins followed by orexin-A induction measured every 1 sec by FLIPR assay
[PMID: 26045032]
体外実験

Orexins are released in a Ca2+-sensitive manner at axonal terminals and can then bind to two closely related G-protein-coupled receptors (GPCRs): orexin receptor type 1 (OX1) and orexin receptor type 2 (OX2)[1].
ACT-462206 shows binding affinity with Kbs of 17 nM (hOX1), 2.4 nM (hOX2), 28 nM (rOX1), 9.9 nM (rOX2), 27 nM (dOX1), 4.2 nM (dOX2), respectively[1].
ACT-462206 inhibits Orexin activity with IC50s of 60 nM (hOX1), 11 nM (hOX2), 48 nM (rOX1), 9.6 nM (rOX2), 68 nM (dOX1), 26 nM (dOX2), respectively[1].
ACT-462206 inhibits CYP450 3A4T and 3A4M with IC50s of 15 μM and 29 μM, respectively[1].

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

ACT-462206 関連抗体
体内実験

ACT-462206 (compound 24) (100 mg/kg; p.o.; sampling at 3 h) can go cross blood brain barrier, with concentrations are 2267 ng/mL and 1219 ng/g in plasma and brain, respectively in male Wistar rats[1].
ACT-462206 (10-300 mg/kg; p.o.; single dose) shows sleep-promoting effects in male Wistar rats and in male Beagle dogs, with decreasing wakefulness and increasing non-rapid eye movement (non-REM) and REM sleep[1].
ACT-462206 (100, 300 mg/kg; p.o.; single dose) exerts anxiolytic-like effects, decreases the fear-potentiated startle reflexes in response to a sudden loud noise in rats, reduces the socialstress-induced increases of locomotion, body temperature, and heart rate[1].
Pharmacokinetics in different species[1]

Route Dose (mg/kg) AUC (ng h/mL) CL (mL/min/kg) Vss (L/kg) t1/2 (h) cmax (ng/mL) tmax (h) F1/2 (%)
rat i.v. 1 586 29 1.8 1.9 / / /
p.o. 10 2310 / / / 1600 0.5 39
dog i.v. 1 1490 11 1.4 1.7 / / /
p.o. 3 2750 / / / 426 0.5 52

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

Animal Model: Male Wistar rats[1]
Dosage: 0, 10, 30, 100, 300 mg/kg
Administration: Oral gavage; single dose
Result: Decreased the latency to the first persistent episode of non-REM sleep (60 s) and the first persistent episode of REM sleep (30 s).
Dose-dependently decreased total wake time and behavioral home cage activity (one-way ANOVA; p <0.001), while increasing REM and non-REM sleep times.
臨床実験
分子量

388.48

分子式

C20H24N2O4S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(S(=O)(C2=CC=C(OC)C=C2)=O)CCC1)NC3=CC(C)=CC(C)=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (257.41 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 2.5741 mL 12.8707 mL 25.7414 mL
5 mM 0.5148 mL 2.5741 mL 5.1483 mL
10 mM 0.2574 mL 1.2871 mL 2.5741 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます：C1V1 = C2V2

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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: ≥ 2.5 mg/mL (6.44 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 (6.44 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 (protect from light)

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
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 (protect from light). 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 2.5741 mL 12.8707 mL 25.7414 mL 64.3534 mL
5 mM 0.5148 mL 2.5741 mL 5.1483 mL 12.8707 mL
10 mM 0.2574 mL 1.2871 mL 2.5741 mL 6.4353 mL
15 mM 0.1716 mL 0.8580 mL 1.7161 mL 4.2902 mL
20 mM 0.1287 mL 0.6435 mL 1.2871 mL 3.2177 mL
25 mM 0.1030 mL 0.5148 mL 1.0297 mL 2.5741 mL
30 mM 0.0858 mL 0.4290 mL 0.8580 mL 2.1451 mL
40 mM 0.0644 mL 0.3218 mL 0.6435 mL 1.6088 mL
50 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2871 mL
60 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0726 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8044 mL
100 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6435 mL
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ACT-462206 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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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:

ACT-4622061361321-96-1ACT462206ACT 462206Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT Receptorproline sulfonamideOrexinbrain-penetrantinsomniaanxiety-related disordersaddictionblood brain barrierInhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-101834
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