[CAS NO. 298690-60-5] Ro 67-7476
PRODUCTS SPECIFICATIONS [298690-60-5]
DESCRIPTION [298690-60-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 319.39 |
| Molecular Formula | C17H18FNO2S |
| SMILES | O=S(N1[C@H](C2=CC=C(F)C=C2)CCC1)(C3=CC=C(C)C=C3)=O |
3 Publications Citing Use of MCE
Summary
Ro 67-7476 is a potent positive allosteric modulator of mGluR 1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC 50 of 60.1 nM [1] [2] . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate ( EC 50 =163.3 nM) [3] .
IC50 & Target
|
mGluR1a 60.1 nM (EC 50 ) |
In Vitro
In the Purkinje cells of rat cerebellar slices, Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5
[3]
.
Ro 67-7476 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC
50
=163.3 nM). The EC50 value of full P-ERK1/2 activation for Ro 67-7476 are nearly identical to the EC
50
for calcium mobilization potentiation
[3]
.
Ro 67-7476 increases basal cAMP production approximately by 8%. It potentiated threshold responses to glutamate in the cAMP accumulation assay, with an EC
50
value of 17.7 µM
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : ≥ 40 mg/mL ( 125.24 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1310 mL | 15.6548 mL | 31.3097 mL |
| 5 mM | 0.6262 mL | 3.1310 mL | 6.2619 mL |
| 10 mM | 0.3131 mL | 1.5655 mL | 3.1310 mL |
References
- [1] F Knoflach, et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7
- [2] Kamondanai Hemstapat, et al. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol Pharmacol. 2006 Aug;70(2):616-26.
- [3] Douglas J Sheffler, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008 Sep;55(4):419-27