Ro 67-4853
Based on 1 Customer Validation
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.
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- Pureté: 99.90%
- CAS No.: 302841-89-0
- Formule: C19H19NO4
- Masse moléculaire:325.36
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Rat mGluR1a 7.16 (pEC50) |
Ro67-4853 selectively potentiates responses to the agonist DHPG[2].
Ro 67-4853 (1 µM) shifts the concentration-response curve (CRC) of glutamate approximately 2-fold, 15-fold, and 4.5-fold to the left respectively in BHK cells stably expressing mGluR1a[4].
Ro 67-4853 (1 µM) activates p-ERK1/2 in the absence of agonist with a time course of activation peaking at 5 minutes in BHK cells[4].
Ro 67-4853 (500 nM) potentiates glutamate-induced activation of mGluR1 as assessed by measures of cAMP production. Glutamate increases cAMP accumulation with an EC50 value of 32.08 µM in the absence of Ro 67-4853. The EC50 values for glutamate in the presence of Ro 67-4853 is 2.15 µM. Ro 67-4853 increases basal mGluR1-induced cAMP accumulation and potentiate glutamate-induced cAMP accumulation but have lower potencies at modulating the cAMP response than at regulating ERK1/2 phosphorylation or calcium mobilization[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 302841-89-0
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Appearance Solid
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Masse moléculaire 325.36
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Formule C19H19NO4
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Color White to off-white
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SMILES
CCCCOC(NC(C1C2=CC=CC=C2OC3=CC=CC=C13)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMF : 16 mg/mL (49.18 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (701 KB)
- English - EN (701 KB)
- Français - FR (701 KB)
- Deutsch - DE (701 KB)
- Norwegian - NO (701 KB)
- Español - ES (701 KB)
- Swedish - SV (701 KB)
- Italian - IT (701 KB)
- Korean - KR (701 KB)
- Portuguese - PT (701 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Knoflach F, et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site [published correction appears in Proc Natl Acad Sci U S A 2001 Dec 18;98(26):15393]. Proc Natl Acad Sci U S A. [Content Brief]
[2]. Jiang JY, et al. Extracellular calcium modulates actions of orthosteric and allosteric ligands on metabotropic glutamate receptor 1α. J Biol Chem. 2014;289(3):1649-1661. [Content Brief]
[3]. Salt TE, et al. Potentiation of sensory responses in ventrobasal thalamus in vivo via selective modulation of mGlu1 receptors with a positive allosteric modulator. Neuropharmacology. 2012;62(4):1695-1699. [Content Brief]
[4]. Sheffler DJ, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008;55(4):419-427. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF | 1 mM | 3.0735 mL | 15.3676 mL | 30.7352 mL | 76.8380 mL |
| 5 mM | 0.6147 mL | 3.0735 mL | 6.1470 mL | 15.3676 mL | |
| 10 mM | 0.3074 mL | 1.5368 mL | 3.0735 mL | 7.6838 mL | |
| 15 mM | 0.2049 mL | 1.0245 mL | 2.0490 mL | 5.1225 mL | |
| 20 mM | 0.1537 mL | 0.7684 mL | 1.5368 mL | 3.8419 mL | |
| 25 mM | 0.1229 mL | 0.6147 mL | 1.2294 mL | 3.0735 mL | |
| 30 mM | 0.1025 mL | 0.5123 mL | 1.0245 mL | 2.5613 mL | |
| 40 mM | 0.0768 mL | 0.3842 mL | 0.7684 mL | 1.9209 mL |
Ro 67-4853 Related Classifications
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