2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Apoptosis
  3. Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis
  4. Almorexant

Almorexant  (Synonyms: ACT 078573)

製品番号: HY-10805 純度: 99.96%
COA 取扱説明書 Technical Support

Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd 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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CAS 番号 : 871224-64-5

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 125 在庫あり
Solution
10 mM * 1 mL in DMSO USD 125 在庫あり
Solid
5 mg $111 在庫あり
10 mg $178 在庫あり
25 mg $416 在庫あり
50 mg $666 在庫あり
100 mg $1000 在庫あり
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カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Other Forms of Almorexant:

Almorexant 関連抗体

Top Publications Citing Use of Products

    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

    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

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

    Caspase 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
    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

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd 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[1][2][3][4].

    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
    13 nM
    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
    13 nM
    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 nM
    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
    8 nM
    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]
    体外実験

    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.

    Almorexant 関連抗体
    体内実験

    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.
    分子量

    512.56

    分子式

    C29H31F3N2O3
    CAS 番号
    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
    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 (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.

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    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

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    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:

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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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    +
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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).
    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: 99.96%

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

    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
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    Almorexant 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）
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    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:

    Almorexant871224-64-5ACT 078573ACT078573ACT-078573Orexin Receptor (OX Receptor)Calcium ChannelCaspaseApoptosisHypocretin ReceptorHCRT ReceptorCa2+ channelsCa channelsAsPC-1 cellsHPAF-II cellsPancreatic ductal adenocarcinomaPDACGPCRapoptosispancreatic cancernarcolepsyorexinhypocretinCataplexyInhibitorinhibitorinhibit

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    製品番号:
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