1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. GV-58

GV-58 

Cat. No.: HY-12498 Purity: 99.51%
Handling Instructions

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.

For research use only. We do not sell to patients.

GV-58 Chemical Structure

GV-58 Chemical Structure

CAS No. : 1402821-41-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 297 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 297 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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 agonist 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 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.

Molecular Weight

374.50

Formula

C18H26N6OS

CAS No.
SMILES

CC[[email protected]@H](NC1=NC(NCC2=CC=C(C)S2)=C3N=CN(CCC)C3=N1)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (267.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6702 mL 13.3511 mL 26.7023 mL
5 mM 0.5340 mL 2.6702 mL 5.3405 mL
10 mM 0.2670 mL 1.3351 mL 2.6702 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.51%

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GV-58
Cat. No.:
HY-12498
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