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GSK-1016790A - 98%, high purity , CAS No.942206-85-1, Activator of TRPV4

In stock
Item Number
G275374
Grouped product items
SKU Size
Availability
Price Qty
G275374-5mg
5mg
5
$81.90
G275374-10mg
10mg
5
$140.90
G275374-25mg
25mg
3
$303.90
G275374-50mg
50mg
3
$538.90

Novel, potent TRPV4 channel agonist

Basic Description

Synonyms GSK101 | HY-19608 | GSK 1016790A | N-[(2S)-1-[4-[(2S)-2-[(2,4-dichlorophenyl)sulfonylamino]-3-hydroxypropanoyl]piperazin-1-yl]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide | AC-33152 | GTPL4205 | IVYQPSHHYIAUFO-VXKWHMMOSA-N | N-[(2S)-1-{4-[N-
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms Novel, potent TRPV4 channel agonist. Induced Ca 2+ influx in mouse and human TRPV4 expressing HEK cells (EC 50 values of 18 and 2.1 nM respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type ACTIVATOR
Mechanism of action Activator of TRPV4
Note Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

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。

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organic acids and derivatives
Class Carboxylic acids and derivatives
Subclass Amino acids, peptides, and analogues
Intermediate Tree Nodes Amino acids and derivatives - Alpha amino acids and derivatives
Direct Parent Leucine and derivatives
Alternative Parents N-acyl-alpha amino acids and derivatives  Alpha amino acid amides  Benzenesulfonamides  1-benzothiophenes  Benzenesulfonyl compounds  Thiophene carboxamides  2,3,5-trisubstituted thiophenes  2-heteroaryl carboxamides  Dichlorobenzenes  Piperazines  Organosulfonamides  Aryl chlorides  Tertiary carboxylic acid amides  Aminosulfonyl compounds  Heteroaromatic compounds  Secondary carboxylic acid amides  Azacyclic compounds  Organic oxides  Organochlorides  Organonitrogen compounds  Hydrocarbon derivatives  Carbonyl compounds  Primary alcohols  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Leucine or derivatives - N-acyl-alpha amino acid or derivatives - Alpha-amino acid amide - Benzenesulfonamide - Benzothiophene - 1-benzothiophene - Benzenesulfonyl group - 2-heteroaryl carboxamide - 1,3-dichlorobenzene - Thiophene carboxamide - 2,3,5-trisubstituted thiophene - Thiophene carboxylic acid or derivatives - Chlorobenzene - Halobenzene - Aryl chloride - Aryl halide - Monocyclic benzene moiety - 1,4-diazinane - Piperazine - Organosulfonic acid amide - Benzenoid - Thiophene - Aminosulfonyl compound - Tertiary carboxylic acid amide - Sulfonyl - Organosulfonic acid or derivatives - Heteroaromatic compound - Organic sulfonic acid or derivatives - Secondary carboxylic acid amide - Carboxamide group - Organoheterocyclic compound - Azacycle - Organic oxygen compound - Alcohol - Hydrocarbon derivative - Organohalogen compound - Carbonyl group - Organic oxide - Organonitrogen compound - Organooxygen compound - Organosulfur compound - Organic nitrogen compound - Primary alcohol - Organochloride - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as leucine and derivatives. These are compounds containing leucine or a derivative thereof resulting from reaction of leucine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
External Descriptors Not available

Associated Targets(Human)

TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
TRPV1 Tclin Vanilloid receptor (8273 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 (774 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 488200359
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/488200359
IUPAC Name N-[(2S)-1-[4-[(2S)-2-[(2,4-dichlorophenyl)sulfonylamino]-3-hydroxypropanoyl]piperazin-1-yl]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide
INCHI InChI=1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1
InChIKey IVYQPSHHYIAUFO-VXKWHMMOSA-N
Smiles CC(C)CC(C(=O)N1CCN(CC1)C(=O)C(CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3
Isomeric SMILES CC(C)C[C@@H](C(=O)N1CCN(CC1)C(=O)[C@H](CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3
Molecular Weight 655.61
Reaxy-Rn 32640315
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=32640315&ln=

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

9 results found

Lot Number Certificate Type Date Item
C2331444 Certificate of Analysis Jul 09, 2025 G275374
C2331427 Certificate of Analysis Jul 09, 2025 G275374
C2331426 Certificate of Analysis Jul 09, 2025 G275374
C2527057 Certificate of Analysis Apr 16, 2025 G275374
C2331455 Certificate of Analysis Feb 01, 2024 G275374
C2331454 Certificate of Analysis Jan 15, 2024 G275374
C2331450 Certificate of Analysis Jan 15, 2024 G275374
C2331456 Certificate of Analysis Jan 12, 2024 G275374
C2331423 Certificate of Analysis Jan 12, 2024 G275374

Chemical and Physical Properties

Solubility DMSO: >10 mg/mL
Molecular Weight 655.600 g/mol
XLogP3 4.400
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 10
Exact Mass 654.114 Da
Monoisotopic Mass 654.114 Da
Topological Polar Surface Area 173.000 Ų
Heavy Atom Count 42
Formal Charge 0
Complexity 1070.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 2
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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