TargetMol

GSK2798745

Product Code:
 
TAR-T15434
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T15434-5mg5mg£534.00
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TAR-T15434-50mg50mg£2,464.00
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Quantity:
TAR-T15434-100mg100mg£3,283.00
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This product comes from: United States.
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Further Information

Bioactivity:
GSK2798745 is an orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker (IC50s: 1.8 and 1.6 nM for hTRPV4 and rTRPV4). It is used in research for the treatment of pulmonary edema associated with congestive heart failure.
CAS:
1419609-94-1
Formula:
C25H28N6O3
Molecular Weight:
460.538
Pathway:
Membrane transporter/Ion channel
Purity:
0.98
SMILES:
CC(C)(O)c1cnc(cn1)N1C[C@@]2(CCC[C@](C)(Cn3cnc4ccc(cc34)C#N)C2)OC1=O
Target:
TRP/TRPV Channel

References

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.