| Identification | Back Directory | [Name]
GV-58 | [CAS]
1402821-41-3 | [Synonyms]
GV-58
GV-58 >=97% (HPLC)
(2R)-2-[[6-[[(5-Methylthiophen-2-yl)methyl]amino]-9-propyl-9H-purin-2-yl]amino]butan-1-ol
1-Butanol, 2-[[6-[[(5-methyl-2-thienyl)methyl]amino]-9-propyl-9H-purin-2-yl]amino]-, (2R)- | [Molecular Formula]
C18H26N6OS | [MDL Number]
MFCD28385865 | [MOL File]
1402821-41-3.mol | [Molecular Weight]
374.5 |
| Chemical Properties | Back Directory | [Boiling point ]
599.6±60.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (133.51 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
solid | [pka]
14.56±0.10(Predicted) | [color ]
White to off-white | [InChI]
1S/C18H26N6OS/c1-4-8-24-11-20-15-16(19-9-14-7-6-12(3)26-14)22-18(23-17(15)24)21-13(5-2)10-25/h6-7,11,13,25H,4-5,8-10H2,1-3H3,(H2,19,21,22,23)/t13-/m1/s1 | [InChIKey]
DPTXJOUVBMUSGY-CYBMUJFWSA-N | [SMILES]
CCCN1C2=NC(N[C@H](CC)CO)=NC(NCC3=CC=C(C)S3)=C2N=C1 |
| Hazard Information | Back Directory | [Uses]
GV-58 is a novel N- and P/Q-type calcium (Ca2+) channel agonist with EC50s of 7.21 and 8.81 μM, respectively. GV-58 slows the deactivation of channels, resulting in a large increase in presynaptic Ca2+ entry during activity. GV-58 can be used in lambert-eaton myasthenic syndrome (LEMS) research[1][2][3]. | [Biological Activity]
GV-58 is a roscovitine analog th at retains the ability to prolong the open state of calcium channelsbut unlike roscovitineis inactive against Cdk activity. GV-58 is a selective agonist of N-type and P/Q type calcium channelswhich are critical to the triggering of neurotransmitter release at the neuromuscular junction. GV-58 has been studied as a possible therapeutic agent in a mouse model of Lambert-Eaton myasthenic syndrome (LEMS). The EC50 values for activation of N-P/Q- and L- type calcium channels are 6.89.9 and >100 μMrespectively. | [IC 50]
N-type calcium channel: 7.21 μM (EC50); P/Q-type calcium?channel: 8.81 μM (EC50) | [storage]
+4°C | [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. DOI:10.1523/JNEUROSCI.4629-12.2013
[2] Tarr TB, et al. Complete reversal of Lambert-Eaton myasthenic syndrome synaptic impairment by the combined use of a K+ channel blocker and a Ca2+ channel agonist. J Physiol. 2014 Aug 15;592(16):3687-96. DOI:10.1113/jphysiol.2014.276493
[3] Meriney SD, et al. Lambert-Eaton myasthenic syndrome: mouse passive-transfer model illuminates disease pathology and facilitates testing therapeutic leads. Ann N Y Acad Sci. 2018 Jan;1412(1):73-81. DOI:10.1111/nyas.13512 |
|
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|