1402821-41-3

1402821-41-3 structure

Name: GV-58
Chemical Name: (2R)-2-[(6-{[(5-methylthiophen-2-yl)methyl]amino}-9-propyl-9H-purin-2-yl)amino]butan-1-ol
CAS Number: 1402821-41-3
Molecular Formula: C₁₈H₂₆N₆OS
Molecular Weight: 374.504
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
Create Date: 2018-02-20 14:31:45
Modify Date: 2024-01-02 13:58:20
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.IC50 value: 7.21/8.81 uM (N-type/P-Q-type Ca2+ channel) [1]Target: Ca2+ channel agonistIn comparison with the parent molecule, (R)-roscovitine, GV-58 has a 20-fold less potent cyclin-dependent kinase antagonist effect, a 3- to 4-fold more potent Ca2+ channel agonist effect, and 4-fold higher efficacy as a Ca2+ channel agonist. GV-58 had no agonist activity (up to 100 μm) on the L-type α-subunit we tested (Cav1.3). In summary, GV-58 greatly improved upon (R)-roscovitine in terms of our properties of interest, with a ～4-fold increase in efficacy as an agonist for N- and P/Q-type Ca2+ channels, a ～3- to 4-fold increase in potency as an agonist for N- and P/Q-type Ca2+ channels, and a 20-fold decrease in potency as a Cdk antagonist.

Name	(2R)-2-[(6-{[(5-methylthiophen-2-yl)methyl]amino}-9-propyl-9H-purin-2-yl)amino]butan-1-ol
Synonyms	1-Butanol, 2-[[6-[[(5-methyl-2-thienyl)methyl]amino]-9-propyl-9H-purin-2-yl]amino]-, (2R)- (2R)-2-[(6-{[(5-Methyl-2-thienyl)methyl]amino}-9-propyl-9H-purin-2-yl)amino]-1-butanol gv-58,gv58 GV-58

Description	GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.IC50 value: 7.21/8.81 uM (N-type/P-Q-type Ca2+ channel) [1]Target: Ca2+ channel agonistIn comparison with the parent molecule, (R)-roscovitine, GV-58 has a 20-fold less potent cyclin-dependent kinase antagonist effect, a 3- to 4-fold more potent Ca2+ channel agonist effect, and 4-fold higher efficacy as a Ca2+ channel agonist. GV-58 had no agonist activity (up to 100 μm) on the L-type α-subunit we tested (Cav1.3). In summary, GV-58 greatly improved upon (R)-roscovitine in terms of our properties of interest, with a ～4-fold increase in efficacy as an agonist for N- and P/Q-type Ca2+ channels, a ～3- to 4-fold increase in potency as an agonist for N- and P/Q-type Ca2+ channels, and a 20-fold decrease in potency as a Cdk antagonist.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Neurological Disease
References	[1]. Tarr TB, et al. Evaluation of a novel calcium channel agonist for therapeutic potential in Lambert-Eaton myasthenic syndrome. J Neurosci. 2013 Jun 19;33(25):10559-67.

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319
Precautionary Statements	P305 + P351 + P338
RIDADR	NONH for all modes of transport