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GSK2798745
SKU
HY-19765-10 mg
Category Reference compound
Tags Cardiovascular Disease, Membrane Transporter/Ion Channel;Neuronal Signaling, TRP Channel
$695 – $3,750
Products Details
Product 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].
Web ID
– HY-19765
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C25H28N6O3
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.|[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.
CAS Number
– 1419609-94-1
Molecular Weight
– 460.53
Compound Purity
– 99.71
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
Clinical Information
– Phase 2
Research Area
– Cardiovascular Disease
Solubility
– DMSO : 250 mg/mL (ultrasonic)
Target
– TRP Channel
Pathway
– Membrane Transporter/Ion Channel;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.