GV-58

Modify Date: 2024-01-02 13:58:20

GV-58 Structure
GV-58 structure
Common Name GV-58
CAS Number 1402821-41-3 Molecular Weight 374.504
Density 1.3±0.1 g/cm3 Boiling Point 599.6±60.0 °C at 760 mmHg
Molecular Formula C18H26N6OS Melting Point N/A
MSDS Chinese USA Flash Point 316.4±32.9 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of GV-58


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.

 Names

Name (2R)-2-[(6-{[(5-methylthiophen-2-yl)methyl]amino}-9-propyl-9H-purin-2-yl)amino]butan-1-ol
Synonym More Synonyms

 GV-58 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 599.6±60.0 °C at 760 mmHg
Molecular Formula C18H26N6OS
Molecular Weight 374.504
Flash Point 316.4±32.9 °C
Exact Mass 374.188873
PSA 116.13000
LogP 2.01
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.674
Storage condition 2-8℃

 Safety Information

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

 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
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: GV-58
  • Price: $1100.0/100mg $2200.0/250mg $4400.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: $297/10mM*1mLinDMSO

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