GSK1016790A( GSK1016790A | GSK-1016790A | GSK 1016790A. )

Catalog No. M19275 CAS No. 942206-85-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK1016790A
Note

Research use only, not for human use.
Brief Description

GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.
Description

GSK1016790A is a TRPV4 agonist that elicits calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively).
In Vitro

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In Vivo

Animal Model:S100β-GFP and TRPV4 knockout (TRPV4-/-) mice Dosage:0.001, 0.01, 0.1 mg/kg Administration:IP; single dose Result:Produced a dose-dependent inhibitory effect on whole gut transit time in mice.Produced a dose-dependent and time-dependent inhibitory effect on colonic expulsion.
Synonyms

GSK1016790A | GSK-1016790A | GSK 1016790A.
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

hTRPV4| mTRPV4
Research Area

Cancer
Indication

——

CAS Number

942206-85-1
Formula Weight

655.61
Molecular Formula

C28H32Cl2N4O6S2
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 33 mg/mL; 50.33 mM
SMILES

CC(C)C[C@H](NC(=O)C1=CC2=C(S1)C=CC=C2)C(=O)N1CCN(CC1)C(=O)[C@H](CO)NS(=O)(=O)C1=C(Cl)C=C(Cl)C=C1
Chemical 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