Synonym
Ro64-5229; Ro64-5229; Ro64-5229.
IUPAC/Chemical Name
1-[(Z)-2-cycloheptyloxy-2-(2,6-dichlorophenyl)ethenyl]-1,2,4-triazole
InChi Key
STCVFKBRXOEQRF-YBEGLDIGSA-N
InChi Code
InChI=1S/C17H19Cl2N3O/c18-14-8-5-9-15(19)17(14)16(10-22-12-20-11-21-22)23-13-6-3-1-2-4-7-13/h5,8-13H,1-4,6-7H2/b16-10-
SMILES Code
ClC1=C(/C(OC2CCCCCC2)=C/N3N=CN=C3)C(Cl)=CC=C1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and ethanol
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Ro64-5229 inhibits GTPγ35S binding to mGlu2-containing membranes (IC50 = 0.11 μM).
In vitro activity:
To be determined
In vivo activity:
RO 64-5229 reduces the presynaptic inhibitory effect of Neuroligin 1
Reference: Front Mol Neurosci. 2017 May 3;10:116. https://pubmed.ncbi.nlm.nih.gov/28515678/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
35.2 |
100.00 |
| Ethanol |
35.2 |
100.00 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
352.26
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Gjørlund MD, Carlsen EMM, Kønig AB, Dmytrieva O, Petersen AV, Jacobsen J, Berezin V, Perrier JF, Owczarek S. Soluble Ectodomain of Neuroligin 1 Decreases Synaptic Activity by Activating Metabotropic Glutamate Receptor 2. Front Mol Neurosci. 2017 May 3;10:116. doi: 10.3389/fnmol.2017.00116. PMID: 28515678; PMCID: PMC5413576.
In vitro protocol:
To be determined
In vivo protocol:
1. Gjørlund MD, Carlsen EMM, Kønig AB, Dmytrieva O, Petersen AV, Jacobsen J, Berezin V, Perrier JF, Owczarek S. Soluble Ectodomain of Neuroligin 1 Decreases Synaptic Activity by Activating Metabotropic Glutamate Receptor 2. Front Mol Neurosci. 2017 May 3;10:116. doi: 10.3389/fnmol.2017.00116. PMID: 28515678; PMCID: PMC5413576.
1. Brauner-Osbourne et al (2007) Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors. Curr.Drug Targets. 8 169. PMID: 17266540.
2. Kolczewski et al (1999) Synthesis of heterocyclic enol ethers and their use as a group 2 metabotropic glutamate receptor antagonists. Bioorg.Med.Chem.Lett. 9 2173. PMID: 10465539.
3: Doumazane, E., Scholler, P., Fabre, L., Zwier, J. M., Trinquet, E., Pin, J. P., & Rondard, P. (2013). Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors. Proceedings of the National Academy of Sciences, 110(15), E1416-E1425.
4:Cao, A. M., Quast, R. B., Fatemi, F., Rondard, P., Pin, J. P., & Margeat, E. (2021). Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state. Nature Communications, 12(1), 5426.
