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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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G275374-5mg
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5mg |
5
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$81.90
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G275374-10mg
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10mg |
5
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$140.90
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G275374-25mg
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25mg |
3
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$303.90
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G275374-50mg
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50mg |
3
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$538.90
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Novel, potent TRPV4 channel agonist
| 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。 |
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 |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| 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= |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
| Certificate of Analysis | Jul 09, 2025 | G275374 | |
| Certificate of Analysis | Jul 09, 2025 | G275374 | |
| Certificate of Analysis | Jul 09, 2025 | G275374 | |
| Certificate of Analysis | Apr 16, 2025 | G275374 | |
| Certificate of Analysis | Feb 01, 2024 | G275374 | |
| Certificate of Analysis | Jan 15, 2024 | G275374 | |
| Certificate of Analysis | Jan 15, 2024 | G275374 | |
| Certificate of Analysis | Jan 12, 2024 | G275374 | |
| Certificate of Analysis | Jan 12, 2024 | G275374 |
| 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 |