2. GPCR/G Protein Membrane Transporter/Ion Channel
  3. Potassium Channel LPL Receptor
  4. Siponimod

シポニモド  (Synonyms: Siponimod; BAF-312)

製品番号: HY-12355 純度: 99.95%
COA 取扱説明書 Technical Support

Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1230487-00-9

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 75 在庫あり
Solution
10 mM * 1 mL in DMSO USD 75 在庫あり
Solid
5 mg $66 在庫あり
10 mg $99 在庫あり
25 mg $160 在庫あり
50 mg $286 在庫あり
100 mg $396 在庫あり
500 mg $1320 在庫あり
1 g $2200 在庫あり
5 g   お問い合わせ  
10 g   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

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

カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of Siponimod:

シポニモド 関連抗体

Top Publications Citing Use of Products

    Siponimod purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2025 Apr:213:138-145.  [Abstract]

    Internalization of S1P1 on microglia treated with siponimod. Representative flow cytometry data showing the internalization of S1P1 on microglia with no treatment (blue) or 1000 nM Siponimod (red).

    Siponimod purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2025 Apr:213:138-145.  [Abstract]

    Western blot and quantification were performed on microglial cell culture lysates and supernatants with or without prior Siponimod (1000 nM) treatment, followed by stimulation with LPS and nigrain.

    Siponimod purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Aug 1;14(1):17823.  [Abstract]

    weight loss was averted in Siponimod (0.45 µg/d) treated mice independent of BDNFko.

    Siponimod purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Aug 1;14(1):17823.  [Abstract]

    Siponimod (0.45 µg/d) treatment reduces lymphocyte infiltration of white matter in lumbar spinal cord. Represenative hematoxylin and eosin (HE) images of spinal cord sections.

    Siponimod purchased from MedChemExpress. Usage Cited in: Vet Microbiol. 2021 Oct:261:109177.

    The S1P-S1P3 axis is involved in the infection of PPV. PK15 cells were infected with PPV (MOI = 1) and simultaneously incubated with 10 μM Fingolimod hydrochloride (FTY720), 10 μM Siponimod (BAF-312), 10 μM TY-52,156 or not for 24 h. The values of Log copy number and Log TCID50 for 24 h p.i. were done.

    LPL 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
    LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

    • 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

    Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis[1][2][3][4].

    IC50 & Target

    S1PR1

    0.39 nM (EC50)

    S1PR5

    0.98 nM (EC50)

    S1PR4

    750 nM (EC50)

    S1PR3

    >1000 nM (EC50)

    S1PR2

    >10000 nM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    0.0004 μM
    Compound: 32, BAF312, Siponimod
    Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
    Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
    		[PMID: 24900670]
    CHO EC50
    0.98 nM
    Compound: 3, BAF312
    Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
    Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
    		[PMID: 24125884]
    CHO EC50
    5 μM
    Compound: 32, BAF312, Siponimod
    Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
    Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
    		[PMID: 24900670]
    CHO EC50
    750 nM
    Compound: 3, BAF312
    Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
    Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
    		[PMID: 24125884]
    体外実験

    Siponimod (10-1000 nM; 4-13 h) induces significant and persistent internalization of human S1P1 receptors in CHO cells. Obvious internalization is detectable even at concentrations as low as 10 nM, and the receptors remain localized intracellularly after drug washout[1].
    Siponimod regulates microglial function by reducing IL6 secretion in cultured microglia[4].
    Siponimod improves oligodendrocyte degeneration by alleviating demyelination in organotypic brain slice cultures[4].

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

    シポニモド 関連抗体
    体内実験

    Siponimod (0.03-3 mg/kg; p.o.; daily; day 11 to day 34 post-immunization) dose-dependently suppresses established chronic experimental autoimmune encephalomyelitis in female DA rats, with significant efficacy observed at doses of 0.3 mg/kg and 3 mg/kg[1].
    Siponimod (0.14-1 mg/kg; p.o.; single dose) causes a rapid, dose-dependent reduction in peripheral lymphocyte counts in Lewis rats, with an ED50 of 0.14 mg/kg at 6 hours post-dose, and counts return to normal within 48 hours[2].

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

    Animal Model: Dark Agouti (DA) (female, 9 weeks old at immunization, 200-250 g, chronic experimental autoimmune encephalomyelitis induced via subcutaneous tail base injection of antigen/adjuvant mix)[1]
    Dosage: 0.03 mg/kg; 0.3 mg/kg; 3 mg/kg
    Administration: p.o.; daily; day 11 to day 34 post-immunization
    Result: Reduced area under the curve (AUC) of clinical disease scores from days 12 to 34 compared with vehicle-treated controls.
    Showed borderline effect on disease scores at 0.03 mg/kg dose.
    Animal Model: Lewis rats[2]
    Dosage: 1 mg/kg; 0.14 mg/kg
    Administration: p.o.; single dose
    Result: Decreased peripheral lymphocyte counts by 88% at 8 hours post-administration.
    Returned peripheral lymphocyte counts to normal levels by 48 hours post-administration.
    Achieved an ED50 of 0.14 mg/kg for 50% reduction of peripheral lymphocyte counts at 6 hours post-dose.
    臨床実験
    分子量

    516.60

    分子式

    C29H35F3N2O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1CN(CC2=CC=C(/C(C)=N/OCC3=CC=C(C4CCCCC4)C(C(F)(F)F)=C3)C=C2CC)C1)O
    輸送条件

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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    DMSO : 25 mg/mL (48.39 mM; ultrasonic and warming and heat to 60°C; 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 1.9357 mL 9.6787 mL 19.3573 mL
    5 mM 0.3871 mL 1.9357 mL 3.8715 mL
    10 mM 0.1936 mL 0.9679 mL 1.9357 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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: ≥ 2.5 mg/mL (4.84 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 (4.84 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
    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).

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    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: 99.95%

    COA (245 KB) HNMR (283 KB) LCMS (134 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9357 mL 9.6787 mL 19.3573 mL 48.3933 mL
    5 mM 0.3871 mL 1.9357 mL 3.8715 mL 9.6787 mL
    10 mM 0.1936 mL 0.9679 mL 1.9357 mL 4.8393 mL
    15 mM 0.1290 mL 0.6452 mL 1.2905 mL 3.2262 mL
    20 mM 0.0968 mL 0.4839 mL 0.9679 mL 2.4197 mL
    25 mM 0.0774 mL 0.3871 mL 0.7743 mL 1.9357 mL
    30 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6131 mL
    40 mM 0.0484 mL 0.2420 mL 0.4839 mL 1.2098 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Siponimod 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:

    Siponimod1230487-00-9BAF-312BAF312BAF 312Potassium ChannelLPL ReceptorKcsALysophospholipid Receptormultiple sclerosisneurodegenerationinflammationsiponimodprogressiveS1P receptorS1P1 agonistlymphocytesInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Siponimod
    製品番号:
    HY-12355
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.