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
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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. |
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| Related Catalog | |
| References |
| 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℃ |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319 |
| Precautionary Statements | P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |