2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. GSK205

GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca2+ influx.

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CAS No. : 1263068-83-2

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무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 13 publication(s) in Google Scholar

GSK205 Related Antibodies

Top Publications Citing Use of Products

    GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891.  [Abstract]

    LDH release induced by CSE was abrogated by pharmacological inhibition of TRPV4 with GSK 205 (10 μM).

    GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891.  [Abstract]

    Pharmacological inhibition with GSK 205 (10 μM) decreased the level of NLRP3, Pro-Caspase-1, Cleavage cspase-1, GSDMD, GSDMD-N induced by CSE.

    GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891.  [Abstract]

    Pharmacological inhibition with GSK 205 (10 μM) abrogated PI positive cell induced by CSE.

    GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891.  [Abstract]

    Increased IL-8, IL-1β, IL-18 mRNA expression induced by CSE were abrogated by pharmacological inhibition with GSK205 (10 μM).

    View All TRP Channel Isoform Specific Products:

    View All Isoforms
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca2+ influx[1][2].

    IC50 & Target

    TRPV4

    21 μM (EC50)

    TRPV1

    28 μM (EC50)

    In Vitro

    GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist[1].
    GSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes[1].

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

    GSK205 Related Antibodies

    RT-PCR[1]

    Cell Line: T3-F442A adipocytes
    Concentration: 5 μM
    Incubation Time: 4 days
    Result: Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.
    In Vivo

    GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days; for 4 weeks; male C57BL/6J mice) treatment shows significantly increases expression of thermogenic genes such as Ucp1, Pgc1a, Cidea and Cox8b. GSK205 treatment causes a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. GSK205 treatment significantly improves glucose tolerance in diet-induced obese (DIO) mice. There are no apparent sign of sickness or weight loss[1].
    GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues[1].

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

    Animal Model: Male C57BL/6J mice with high-fat diet[1]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; twice daily; for 7 days
    Result: Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.
    분자량

    481.45

    화학식

    C24H25BrN4S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CN(CCC1=CC=C(NC2=NC=C(C3=CC=CN=C3)S2)C=C1)CC4=CC=CC=C4.[H]Br
    선적

    Room temperature in continental US; may vary elsewhere.
    보관

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    용액&용해도
    In Vitro: 

    DMSO : 250 mg/mL (519.26 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 2.0771 mL 10.3853 mL 20.7706 mL
    5 mM 0.4154 mL 2.0771 mL 4.1541 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 몰농도 계산기

    • 농도 희석 계산기

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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: ≥ 2.08 mg/mL (4.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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, 2 years; -20°C, 1 year (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.
    순도&문서

    Purity: 99.47%

    SDS (393 KB)

    COA (246 KB) HNMR (152 KB) LCMS (87 KB)

    Handling Instructions (2659 KB)
    References

    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 (sealed storage, away from moisture). 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 2.0771 mL 10.3853 mL 20.7706 mL 51.9265 mL
    5 mM 0.4154 mL 2.0771 mL 4.1541 mL 10.3853 mL
    10 mM 0.2077 mL 1.0385 mL 2.0771 mL 5.1926 mL
    15 mM 0.1385 mL 0.6924 mL 1.3847 mL 3.4618 mL
    20 mM 0.1039 mL 0.5193 mL 1.0385 mL 2.5963 mL
    25 mM 0.0831 mL 0.4154 mL 0.8308 mL 2.0771 mL
    30 mM 0.0692 mL 0.3462 mL 0.6924 mL 1.7309 mL
    40 mM 0.0519 mL 0.2596 mL 0.5193 mL 1.2982 mL
    50 mM 0.0415 mL 0.2077 mL 0.4154 mL 1.0385 mL
    60 mM 0.0346 mL 0.1731 mL 0.3462 mL 0.8654 mL
    80 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6491 mL
    100 mM 0.0208 mL 0.1039 mL 0.2077 mL 0.5193 mL
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    GSK205 Related Classifications

    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:

    GSK2051263068-83-2GSK 205GSK-205TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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    상품명:
    GSK205
    Cat. No.:
    HY-120691A
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    SAFETY DATA SHEET (SDS)

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