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

Item Number
G275374
Grouped product items
SKUSizeAvailabilityPrice Qty
G275374-5mg
5mg
In stock
$81.90
G275374-10mg
10mg
In stock
$140.90
G275374-25mg
25mg
In stock
$303.90
G275374-50mg
50mg
In stock
$538.90

Novel, potent TRPV4 channel agonist

Basic Description

SynonymsGSK101 | 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 & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsNovel, 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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeACTIVATOR
Mechanism of actionActivator of TRPV4
NoteWherever 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。

Associated Targets(Human)

TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TRPV1 Tclin Vanilloid receptor (8273 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 (774 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid488200359
Pubchem Sid Urlhttps://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
InChi Key IVYQPSHHYIAUFO-VXKWHMMOSA-N
Canonical 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
PubChem CID 23630211
Molecular Weight 655.61

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
C2331455Certificate of AnalysisFeb 01, 2024 G275374
C2331454Certificate of AnalysisJan 15, 2024 G275374
C2331450Certificate of AnalysisJan 15, 2024 G275374
C2331427Certificate of AnalysisJan 15, 2024 G275374
C2331423Certificate of AnalysisJan 12, 2024 G275374
C2331456Certificate of AnalysisJan 12, 2024 G275374
C2331444Certificate of AnalysisJan 03, 2024 G275374
C2331426Certificate of AnalysisJan 03, 2024 G275374

Chemical and Physical Properties

SolubilityDMSO: >10 mg/mL

Related Documents

References

1. Xu S, Liu B, Yin M, Koroleva M, Mastrangelo M, Ture S, Morrell CN, Zhang DX, Fisher EA, Jin ZG.  (2016)  A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis..  Oncotarget,  (25): (37622-37635).  [PMID:27191895] [10.1021/op500134e]

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