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GSK2798745

CAT: 0804-HY-19765-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-19765-01Size:5 mg
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Description
GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research[1][2][3].
CAS Number
1419609-94-1
UNSPSC
12352005
Target
TRP Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
COVID-19-immunoregulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/gsk2798745.html
Purity
99.80
Solubility
DMSO : ≥ 100 mg/mL
Smiles
N#CC1=CC=C2N=CN(C[C@](CCC3)(C)C[C@@]43CN(C5=NC=C(C(C)(O)C)N=C5)C(O4)=O)C2=C1
Molecular Formula
C25H28N6O3
Molecular Weight
460.53
References & Citations
[1]Goyal N, et al. Clinical Pharmacokinetics, Safety, and Tolerability of a Novel, First-in-Class TRPV4 Ion Channel Inhibitor, GSK2798745, in Healthy and Heart Failure Subjects. Am J Cardiovasc Drugs. 2019 Jun;19 (3) :335-342.|[2]Brooks CA, et al. Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4) . ACS Med Chem Lett. 2019 Jul 15;10 (8) :1228-1233.|[3]Xiaoping Xu, et al. Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo. J Pharmacol Exp Ther. 2021 Mar;376 (3) :436-443.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
TRPV4

Chemical Information

Gsk-2798745

GSK2798745 is under investigation in clinical trial NCT03372603 (A Study to Assess the Effectiveness and Side Effects of GSK2798745 in Participants With Chronic Cough).

CAS Number1419609-94-1
PubChem CID71227359
IUPAC Name3-[[(5S,7S)-3-[5-(2-hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl]methyl]benzimidazole-5-carbonitrile
Molecular FormulaC25H28N6O3
Molecular Weight460.5
XLogP2
Topological Polar Surface Area117
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count4
Heavy Atom Count34
Formal Charge0
Complexity844
SMILES
C[C@@]1(CCC[C@]2(C1)CN(C(=O)O2)C3=NC=C(N=C3)C(C)(C)O)CN4C=NC5=C4C=C(C=C5)C#N
InChI
InChI=1S/C25H28N6O3/c1-23(2,33)20-11-28-21(12-27-20)31-15-25(34-22(31)32)8-4-7-24(3,13-25)14-30-16-29-18-6-5-17(10-26)9-19(18)30/h5-6,9,11-12,16,33H,4,7-8,13-15H2,1-3H3/t24-,25-/m0/s1
InChIKey
URCMKDJBULWNAI-DQEYMECFSA-N
Chemical Structure
2D Structure
2D structure of Gsk-2798745
CAS: 1419609-94-1
CID: 71227359
Formula: C25H28N6O3
MW: 460.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight460.5
XLogP32
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count4
Exact Mass460.22228878
Monoisotopic Mass460.22228878
Topological Polar Surface Area117 Ų
Heavy Atom Count34
Formal Charge0
Complexity844
Isotope Atom Count0
Defined Atom Stereocenter Count2
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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