2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. WAY-100635

WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.

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CAS 番号 : 162760-96-5

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Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 78 在庫あり
Solution
10 mM * 1 mL in DMSO USD 78 在庫あり
Solid or liquid
5 mg $71 在庫あり
10 mg $119 在庫あり
25 mg $249 在庫あり
50 mg $429 在庫あり
100 mg $759 在庫あり
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カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Other Forms of WAY-100635:

WAY-100635 関連抗体

Top Publications Citing Use of Products

    WAY-100635 purchased from MedChemExpress. Usage Cited in: iScience. 2025 Nov 25;28(12):114211.  [Abstract]

    Experimental design for in vivo functional validation of 5-HT1A. 5-HT1A activity was inhibited by injection of 5-HT1A antagonist, WAY-100635.

    WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319.

    Effects of 5-HTP (10 mg/kg) and WAY100635 (1 mg/kg) on cognitive behavior and motor functions in healthy mice. The BM performance (learning and probe trials) across groups.

    WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319.

    Effects of 5-HTP (10 mg/kg) and WAY100635 (1 mg/kg) on cognitive behavior and motor functions in healthy mice. NORT discrimination index across group.

    WAY-100635 purchased from MedChemExpress. Usage Cited in: Biomedicines. 2025 Sep 23;13(10):2319.

    Impact of WAY100635 pretreatment on 5-HTP's effects in LPS-induced SAE model. Performance during learning phase of BM between groups.

    WAY-100635 purchased from MedChemExpress. Usage Cited in: Chin Med. 2024 Jun 15;19(1):87.  [Abstract]

    5-HT promoted the inflammation in H9 cells. NC, negative control; 5-HT: 5-HT (10 μM) treatment; Way: 5-HT (10 μM) and Way100635 (10 μM) treatment; Tro: 5-HT (10 μM) and Tropisetron (25 μM) treatment; Way + Tro: 5-HT (10 μM), Way100635 (10 μM) and Tropisetron (25 μM) treatment.

    5-HT 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
    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

    Dopamine 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
    Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

    • 生物活性

    • 純度とドキュメンテーション

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    製品説明

    WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist[1][2][3].

    IC50 & Target

    D4 Receptor

     

    5-HT1A Receptor

     

    5-HT1A Receptor

    8.87 (pIC50)

    5-HT1A Receptor

    9.71 (pA2)

    Cellular Effect
    Cell Line Type Value Description References
    HEK293-EBNA IC50
    0.91 1
    Compound: 1, WAY-100635
    Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
    Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
    		[PMID: 21520940]
    CHO EC50
    7.1 1
    Compound: 1
    Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
    Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
    		[PMID: 15239661]
    CHO EC50
    7.1 1
    Compound: 1
    Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
    Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
    		[PMID: 15239661]
    CHO EC50
    7.1 1
    Compound: 1
    Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
    Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
    		[PMID: 15239661]
    HEK293-EBNA IC50
    0.91 1
    Compound: 1, WAY-100635
    Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
    Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
    		[PMID: 21520940]
    CHO EC50
    7.1 1
    Compound: 1
    Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
    Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells
    		[PMID: 15239661]
    CHO IC50
    7.1 1
    Compound: 4, WAY-100635
    Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
    Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
    		[PMID: 20443629]
    JAR IC50
    > 4500 1
    Compound: 1
    Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
    Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
    		[PMID: 15239661]
    JAR IC50
    >4500 1
    Compound: 1
    Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
    Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
    		[PMID: 15239661]
    CHO IC50
    7.1 1
    Compound: 4, WAY-100635
    Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
    Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
    		[PMID: 20443629]
    HEK293-EBNA IC50
    0.91 1
    Compound: 1, WAY-100635
    Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
    Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting
    		[PMID: 21520940]
    JAR IC50
    > 4500 1
    Compound: 1
    Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
    Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
    		[PMID: 15239661]
    体外実験

    The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors[1].
    WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 receptor (3.3 nM) [1].

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

    WAY-100635 関連抗体
    体内実験

    WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat[2].

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

    Animal Model: Male Sprague-Dawley rats (220-240 g)[2]
    Dosage: 1 mg/kg
    Administration: Subcutaneous injection (Pharmacokinetic study)
    Result: Reduced total abstinence score, increased immobility time and the burying behavior was increased.
    分子量

    422.56

    分子式

    C25H34N4O2
    CAS 番号
    Appearance

    Solid-Liquid Mixture

    Color

    Off-white to light yellow

    SMILES

    O=C(N(C1=NC=CC=C1)CCN2CCN(CC2)C3=CC=CC=C3OC)C4CCCCC4
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Pure form -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 : 66.67 mg/mL (157.78 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 2.3665 mL 11.8326 mL 23.6653 mL
    5 mM 0.4733 mL 2.3665 mL 4.7331 mL
    10 mM 0.2367 mL 1.1833 mL 2.3665 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.

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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 (5.92 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 (5.92 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.
    In Vivo Dissolution Calculator
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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: 99.97%

    COA (249 KB) HNMR (136 KB) RP-HPLC (169 KB) LCMS (236 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 2.3665 mL 11.8326 mL 23.6653 mL 59.1632 mL
    5 mM 0.4733 mL 2.3665 mL 4.7331 mL 11.8326 mL
    10 mM 0.2367 mL 1.1833 mL 2.3665 mL 5.9163 mL
    15 mM 0.1578 mL 0.7888 mL 1.5777 mL 3.9442 mL
    20 mM 0.1183 mL 0.5916 mL 1.1833 mL 2.9582 mL
    25 mM 0.0947 mL 0.4733 mL 0.9466 mL 2.3665 mL
    30 mM 0.0789 mL 0.3944 mL 0.7888 mL 1.9721 mL
    40 mM 0.0592 mL 0.2958 mL 0.5916 mL 1.4791 mL
    50 mM 0.0473 mL 0.2367 mL 0.4733 mL 1.1833 mL
    60 mM 0.0394 mL 0.1972 mL 0.3944 mL 0.9861 mL
    80 mM 0.0296 mL 0.1479 mL 0.2958 mL 0.7395 mL
    100 mM 0.0237 mL 0.1183 mL 0.2367 mL 0.5916 mL
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    WAY-100635 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
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      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:

    WAY-100635162760-96-5WAY100635WAY 1006355-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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    製品名:
    WAY-100635
    製品番号:
    HY-10349
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