| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
Ro01-6128 targets the metabotropic glutamate receptor subtype 1 (mGluR1). It acts as a positive allosteric modulator (PAM), binding to an allosteric site within the receptor's seven-transmembrane domain, distinct from the orthosteric glutamate binding pocket. By binding to this allosteric site, Ro01-6128 potentiates the receptor's response to glutamate without directly activating the receptor itself.
|
|---|---|
| ln Vitro |
Ro01-6128 potentiates glutamate-induced calcium release with an EC50 of 104.2 nM at rat mGluR1a. It produces only a ~2-fold leftward shift in the glutamate response curve, preserving physiological dynamic range. It enables selective ERK1/2 activation (EC50 248 nM) in the absence of glutamate, probing basal mGluR1 tone, and permits pathway-specific titration: calcium vs. cAMP (EC50 21.5 μM), dissecting divergent signaling cascades.
|
| ln Vivo |
Specific in vivo data for Ro01-6128 is not extensively detailed in the available literature. As a prototypical mGluR1 PAM, it has been used as a research tool to study mGluR1 function in various animal models. Its moderate potentiating profile makes it a valuable tool for probing mGluR1-mediated physiological processes without causing over-activation.
|
| Enzyme Assay |
The in vitro activity of Ro01-6128 is assessed using radioligand binding assays and functional calcium mobilization assays. For binding studies, membrane preparations from cells expressing rat mGluR1a are incubated with a labeled ligand in the presence of various concentrations of Ro01-6128. For functional assays, cells expressing mGluR1a are loaded with a calcium-sensitive dye and stimulated with glutamate in the presence of the compound; the potentiation of calcium release is measured.
|
| Cell Assay |
Cell-based assays are used to evaluate Ro01-6128's activity. Cells expressing recombinant mGluR1a (typically HEK-293 or CHO cells) are loaded with a fluorescent calcium indicator. The cells are treated with Ro01-6128 at various concentrations, followed by stimulation with a submaximal concentration of glutamate. The potentiation of the calcium response is measured using a fluorescence plate reader. ERK1/2 phosphorylation can also be measured by Western blot or ELISA.
|
| Animal Protocol |
Ro01-6128 has been used in various in vivo studies to investigate mGluR1 function. In these studies, the compound is typically administered systemically (e.g., intraperitoneally) to rodents, and its effects on behaviors related to motor coordination, synaptic plasticity, and cognition are assessed. Its moderate potentiating profile allows for pathway-specific modulation without over-activation.
|
| ADME/Pharmacokinetics |
Ro01-6128 has a molecular weight of 283.32 g/mol and a molecular formula of C17H17NO3. It is soluble in DMSO and ethanol (up to 100 mM). The powder should be stored at -20°C for long-term stability, or at 0-4°C for short-term use. Purity is typically ≥98%. The compound is a prototypical mGluR1 PAM and serves as a reference tool compound.
|
| Toxicity/Toxicokinetics |
Ro01-6128 is a research compound and its full toxicological profile is not detailed in the available literature. In animal studies, it has been used at various doses without significant adverse effects reported, suggesting it is tolerated at the doses used for pharmacological studies. As with any research chemical, standard safety precautions should be followed when handling the compound.
|
| References | |
| Additional Infomation |
Ro01-6128 (CAS#: 302841-86-7) is a selective positive allosteric modulator (PAM) of mGluR1, discovered by Hoffmann-La Roche. It potentiates glutamate-induced calcium release (EC50 = 104.2 nM) and enables pathway-specific titration of mGluR1 signaling. Ro01-6128 is the prototypical mGluR1 PAM from which later, more potent analogs were derived. It is a valuable research tool for studying mGluR1 function in synaptic plasticity, motor coordination, and cognitive processes.
|
| Molecular Formula |
C17H17NO3
|
|---|---|
| Molecular Weight |
283.33
|
| Exact Mass |
283.12
|
| CAS # |
302841-86-7
|
| Related CAS # |
Ro 01-6128; 302841-86-7
|
| PubChem CID |
9903898
|
| Appearance |
White to light brown solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Index of Refraction |
1.562
|
| LogP |
3.38
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
21
|
| Complexity |
326
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCOC(NC(C(C1=CC=CC=C1)C2=CC=CC=C2)=O)=O
|
| InChi Key |
ILSZPWZFQHSKLW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H17NO3/c1-2-21-17(20)18-16(19)15(13-9-5-3-6-10-13)14-11-7-4-8-12-14/h3-12,15H,2H2,1H3,(H,18,19,20)
|
| Chemical Name |
ethyl N-(2,2-diphenylacetyl)carbamate
|
| Synonyms |
Ro 01-6128; Ro-01-6128; Ro01-6128
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~353.0 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (8.82 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5295 mL | 17.6473 mL | 35.2945 mL | |
| 5 mM | 0.7059 mL | 3.5295 mL | 7.0589 mL | |
| 10 mM | 0.3529 mL | 1.7647 mL | 3.5295 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
