Ro 67-7476

Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).

Product information

CAS Number: 298690-60-5

Molecular Weight: 319.39

Formula: C17H18FNO2S

Chemical Name: (2S)-2-(4-fluorophenyl)-1-(4-methylbenzenesulfonyl)pyrrolidine

Smiles: CC1C=CC(=CC=1)S(=O)(=O)N1CCC[C@H]1C1C=CC(F)=CC=1

InChiKey: DAEHFYNGSSBGSS-KRWDZBQOSA-N

InChi: InChI=1S/C17H18FNO2S/c1-13-4-10-16(11-5-13)22(20,21)19-12-2-3-17(19)14-6-8-15(18)9-7-14/h4-11,17H,2-3,12H2,1H3/t17-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 40 mg/mL (125.24 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. Ro 67-7476 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM). The EC50 value of full P-ERK1/2 activation for Ro 67-7476 are nearly identical to the EC50 for calcium mobilization potentiation. Ro 67-7476 increases basal cAMP production approximately by 8%. It potentiated threshold responses to glutamate in the cAMP accumulation assay, with an EC50 value of 17.7 µM.

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

Products are for research use only. Not for human use.