GV-58
Cat. No. :YN360338
CAS No. :1402821-41-3
86-020-82000279
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order@ubiochem.com| Product Name: | GV-58 |
| CAS NO.: | 1402821-41-3 |
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| Molecular Weight: | 374.50 |
| Molecular Formula: | C₁₈H₂₆N₆OS |
| SMILES: | CC[C@@H](NC1=NC(NCC2=CC=C(C)S2)=C3N=CN(CCC)C3=N1)CO |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| 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. In 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 100μM) 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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