Art. -Nr.: HY-19608

GSK1016790A

38 Cited Publications

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Based on 38 publication(s) in Google Scholar

GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca²⁺ influx and elevate intracellular Ca²⁺ in HEK cells.

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Reinheit: 99.93%
CAS. Nr.: 942206-85-1
Formel: C₂₈H₃₂Cl₂N₄O₆S₂
Molecular Weight:655.61

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK1016790A Chemical Structure

CAS. Nr.: 942206-85-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (38)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca²⁺ influx and elevate intracellular Ca²⁺ in HEK cells^[1]^[2].

IC₅₀ & Target^[1]^[2]

TRPV4

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	49 nM Compound: 1; GSK1016790A	Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay	[PMID: 30629441]

In Vitro

GSK1016790A (0.1-1000 nM) elicits Ca²⁺ influx in mouse and human TRPV4-expressing human embryonic kidney (HEK) cells (EC₅₀ values of 18 and 2.1 nM, respectively) and it evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. GSK1016790A (100 nM) treatment elicits a rapid elevation of intracellular Ca²⁺ in a subset of neurons^[2].

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

In Vivo

GSK1016790A (0.001-0.1 mg/kg; i.p.) produces a dose-dependent inhibitory effect on whole gut transit time in mice^[2].
GSK1016790A (0.1-1000 nM; pretreatment 10 min) significantly inhibits the electrical field stimulation (EFS)-induced twitch contractions in isolated mouse colon strips in a concentration-dependent manner^[2].

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

Animal Model:

S100β-GFP and TRPV4 knockout (TRPV4^-/-) mice^[2]
Dosage:

0.001, 0.01, 0.1 mg/kg
Administration:

IP; single dose
Result:

Produced a dose-dependent inhibitory effect on whole gut transit time in mice.
Produced a dose-dependent and time-dependent inhibitory effect on colonic expulsion.

Chemical Information

CAS. Nr. 942206-85-1
Appearance Solid
Molecular Weight 655.61
Formel C₂₈H₃₂Cl₂N₄O₆S₂
Color White to off-white
SMILES

O=C(C1=CC2=CC=CC=C2S1)N[C@H](C(N3CCN(C([C@@H](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O)CC(C)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (38)

All Cell Migration/Invasion AssayOthersFlow CytometryWBIF

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Journal Impact Factor

Signal Transduct Target Ther

Pulsed electromagnetic fields inhibit atherosclerosis by regulating pyroptosis through membrane tension-mediated mechanosensitive channels. [Abstract]

2025 Nov 28;10(1):388. PMID: 41309549

GSK1016790A purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388. [Abstract]

HC067047 (100 nM, transient administration) blocked both GSK1016790A (80 nM,transient administration) -evoked inward and outward transmembrane currents in HUVEC cells.
Nat Immunol

Lipid asymmetry disruption by XKR8 orchestrates neutrophil extracellular trap formation and inhibits fungal infection. [Abstract]

2026 May;27(5):949-960. PMID: 41781710
Adv Mater

A Highly Adaptable Hydrogen Bond Re-Orientation (HyBRO) Strategy for Multiscale Vasculature Fabrication. [Abstract]

2025 May 9:e2417734. PMID: 40344457
Nat Commun

Biomimetic organo-hydrogels reveal the adipose tissue local mechanical anisotropy regulates ovarian cancer invasion. [Abstract]

2025 Sep 29;16(1):8541. PMID: 41022685
Adv Sci (Weinh)

Structural Pharmacology of TRPV4 Antagonists. [Abstract]

2024 Apr 24:e2401583. PMID: 38659239
Chem Eng J

2025 Nov 19.
Cell Discov

Cancer cells sense solid stress to enhance metastasis by CKAP4 phase separation-mediated microtubule branching. [Abstract]

2024 Nov 12;10(1):114. PMID: 39528501
Cell Death Dis

Inhibition of TRPV4 remodels single cell polarity and suppresses the metastasis of hepatocellular carcinoma. [Abstract]

2023 Jun 28;14(6):379. PMID: 37369706

GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]

MHCC-97H and HCC-LM3 cells were treated with 4 μM GSK1016790A or 8 μM HC067047 for 24 h. Transwell migration assay without Matrigel matrix was detected and the number of transmigrated cells were quantified. Scale bar: 200 μm.

GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]

GSK1016790A (2-8 μM, 24 h). The expression of cytoskeleton-related proteins was measured by western blot.

GSK1016790A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]

The MHCC-97H cells were stimulated with 16 μM GSK1016790A for a brief period of time, and the calcium ion fluorescence intensity was acquired by flow cytometry analysis.
Acta Pharmacol Sin

TRPV4 channel is involved in HSV-2 infection in human vaginal epithelial cells through triggering Ca2+ oscillation. [Abstract]

2023 Apr;44(4):811-821. PMID: 36151392
Br J Pharmacol

ATP release and metabolism by human and guinea pig airways and P2X receptor-dependent effects on bronchopulmonary vagal afferent nerve subtypes. [Abstract]

2025 Nov 2. PMID: 41178173
Br J Pharmacol

Endothelial TRPV4-eNOS coupling as a vital therapy target for treatment of hypertension. [Abstract]

2022 May;179(10):2297-2312. PMID: 34822720
Antioxidants (Basel)

Blocking TRPV4 Ameliorates Osteoarthritis by Inhibiting M1 Macrophage Polarization via the ROS/NLRP3 Signaling Pathway. [Abstract]

2022 Nov 23;11(12):2315. PMID: 36552524
J Agric Food Chem

Bromelain Alleviates Sleep Deprivation-Induced Intestinal Injury via TRPA1/5-HT Axis. [Abstract]

2025 Jul 23;73(29):18153-18164. PMID: 40662381
JCI Insight

Small molecule inhibition rescues the skeletal dysplasia phenotype of Trpv4 mutant mice. [Abstract]

2026 Jan 23;11(2):e182439. PMID: 41574606
Transl Res

TRPV4 in adipose tissue ameliorates diet-induced obesity by promoting white adipocyte browning. [Abstract]

2024 Apr:266:16-31. PMID: 37926276
Acta Physiol

The CaSR/TRPV4 coupling mediates pro-inflammatory macrophage function. [Abstract]

2023 Apr;237(4):e13926. PMID: 36606511
Acs Biomater Sci Eng

Cation Channel Transient Receptor Potential Vanilloid 4 Mediates Topography-Induced Osteoblastic Differentiation of Bone Marrow Stem Cells. [Abstract]

2019 Dec 9;5(12):6520-6529. PMID: 33417804

GSK1016790A purchased from MedChemExpress. Usage Cited in: Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529. [Abstract]

Protein levels of NFATc1 in nuclei of BMSCs cultured on various surfaces with or without GSK101 and RN-1734.

GSK1016790A purchased from MedChemExpress. Usage Cited in: Acs Biomater Sci Eng. 2019 Dec 9;5(12):6520-6529. [Abstract]

Effects of TRPV4 on NFATc1 nuclear localization in BMSCs on MNTs. Micrographs stained for NFATc1 of BMSCs cultured for 7d on (A) PT, (B) PT with TRPV4 agonist (GSK101) , (C) TNT-30, (D)TNT-100, (E) TNT-100 with TRPV4 antagonist (RN-1734). Red fluorescence: NFATc1; Blue fluorescence: nucleus.
J Ethnopharmacol

Magnolol and honokiol target TRPC4 to regulate extracellular calcium influx and relax intestinal smooth muscle. [Abstract]

2022 May 23:290:115105. PMID: 35157953
Front Pharmacol

Role of Serosal TRPV4-Constituted SOCE Mechanism in Secretagogues-Stimulated Intestinal Epithelial Anion Secretion. [Abstract]

2021 Jul 14:12:684538. PMID: 34335254
Exp Neurol

Activation of TRPV4 induces intraneuronal tau hyperphosphorylation via cholesterol accumulation. [Abstract]

2023 Jun:364:114392. PMID: 36990137
J Cell Physiol

Simulated microgravity-induced oxidative stress and loss of osteogenic potential of osteoblasts can be prevented by protection of primary cilia. [Abstract]

2023 Nov;238(11):2692-2709. PMID: 37796139
Cell Calcium

Blockage of transient receptor potential vanilloid 4 prevents postoperative atrial fibrillation by inhibiting NLRP3-inflammasome in sterile pericarditis mice. [Abstract]

2022 Jun;104:102590. PMID: 35439615
Sci Rep

The TRPV4-YAP axis mediates cytoskeletal and extracellular matrix remodeling in trabecular meshwork cells as a novel glaucoma mechanism. [Abstract]

2025 Nov 24;15(1):41644. PMID: 41286165
J Biol Chem

Capsaicin inhibits intestinal Cl- secretion and promotes Na+ absorption by blocking TRPV4 channels in healthy and colitic mice. [Abstract]

2022 May;298(5):101847. PMID: 35314195
Cell Signal

TRPV4 blockade alleviates endoplasmic reticulum stress mediated apoptosis in hypoxia-induced cardiomyocyte injury. [Abstract]

2024 Feb:114:110973. PMID: 37981067
Exp Cell Res

Investigating the effects of TRPV4 and Cav1.2 channels in 3D culture for promoting the differentiation of BMSCs at various stages. [Abstract]

2025 Apr 1;447(1):114515. PMID: 40073957
Mol Hum Reprod

Activation of TRPV4 stimulates transepithelial K+ secretion in rat epididymal epithelium. [Abstract]

2022 Feb 4;28(2):gaac001. PMID: 35040999
Am J Physiol Lung Cell Mol Physiol

Adipose-derived exosomes protect the pulmonary endothelial barrier in ventilator-induced lung injury by inhibiting the TRPV4/Ca2+ signaling pathway. [Abstract]

2020 Apr 1;318(4):L723-L741. PMID: 32073873
J Cancer

Matrix stiffness regulates NPC invasiveness by modulating a mechanoresponsive TRPV4-Nox4-IL-8 signaling axis. [Abstract]

2025 Jan 13;16(4):1324-1334. PMID: 39895789
J Leukoc Biol

Transient receptor potential vanilloid 4 (TRPV4) in neutrophils enhances myocardial ischemia/reperfusion injury. [Abstract]

2023 Sep 1;114(3):266-279. PMID: 37232941
Pain Res Manag

Tuina Alleviates Neuropathic Pain in CCI Rats by Regulating the TRPV4-CaMKII Signaling Pathway in Dorsal Root Ganglion. [Abstract]

2025 Aug 6:2025:3697374. PMID: 40809812
Ultrasound Med Biol

Low-Intensity Pulsed Ultrasound Dynamically Modulates the Migration of BV2 Microglia. [Abstract]

2025 Mar;51(3):494-507. PMID: 39632209
J Cardiovasc Transl Res

Roles of TRPV4 in Regulating Circulating Angiogenic Cells to Promote Coronary Microvascular Regeneration. [Abstract]

2023 Apr;16(2):414-426. PMID: 36103035
Biomed Res Int

Role of TRPV4 in the Diagnosis and Treatment of Helicobacter pylori Infection in Children with Duodenal Ulcers. [Abstract]

2022 Jan 4:2022:2777882. PMID: 35028313
SSRN

2025 Dec 12.
SSRN

2025 Oct 29.
bioRxiv

2024 November 26.
SSRN

2024 Jan 22.

Lösungsmittel & Löslichkeit

In Vitro:

Methanol : 50 mg/mL (76.26 mM; Need ultrasonic)

DMSO : ≥ 33 mg/mL (50.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5253 mL

7.6265 mL

15.2530 mL

5 mM

0.3051 mL

1.5253 mL

3.0506 mL

10 mM

0.1525 mL

0.7626 mL

1.5253 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (3.81 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (3.81 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kevin S Thorneloe, et al. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. [Content Brief]

[2]. J Fichna, et al. Transient receptor potential vanilloid 4 inhibits mouse colonic motility by activating NO-dependent enteric neurotransmission. J Mol Med (Berl). 2015 Dec;93(12):1297-309. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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 / Methanol	1 mM	1.5253 mL	7.6265 mL	15.2530 mL	38.1324 mL
	5 mM	0.3051 mL	1.5253 mL	3.0506 mL	7.6265 mL
	10 mM	0.1525 mL	0.7626 mL	1.5253 mL	3.8132 mL
	15 mM	0.1017 mL	0.5084 mL	1.0169 mL	2.5422 mL
	20 mM	0.0763 mL	0.3813 mL	0.7626 mL	1.9066 mL
	25 mM	0.0610 mL	0.3051 mL	0.6101 mL	1.5253 mL
	30 mM	0.0508 mL	0.2542 mL	0.5084 mL	1.2711 mL
	40 mM	0.0381 mL	0.1907 mL	0.3813 mL	0.9533 mL
	50 mM	0.0305 mL	0.1525 mL	0.3051 mL	0.7626 mL
Methanol	60 mM	0.0254 mL	0.1271 mL	0.2542 mL	0.6355 mL

Keywords

GSK1016790A

38 Cited Publications

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GSK1016790A

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Reprogramming Compound Library

Anti-Cardiovascular Disease Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK1016790A

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (38)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK1016790A

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Reprogramming Compound Library

Anti-Cardiovascular Disease Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK1016790A

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (38)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK1016790A Related Classifications

Art. -Nr.: HY-19608