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

GSK205 

Cat. No.: HY-120691A Purity: 99.91%
COA Handling Instructions

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

For research use only. We do not sell to patients.

GSK205 Chemical Structure

GSK205 Chemical Structure

CAS No. : 1263068-83-2

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Solution
10 mM * 1 mL in DMSO USD 201 In-stock
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ready for reconstitution
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10 mg USD 330 In-stock
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Based on 3 publication(s) in Google Scholar

GSK205 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

IC50: 4.19  μM (TRPV4)[2]
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].

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].

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.
Molecular Weight

481.45

Appearance

Solid

Formula

C24H25BrN4S
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (519.26 mM; Need ultrasonic)

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
10 mM 0.2077 mL 1.0385 mL 2.0771 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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

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