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| Targets |
Ro0711401 targets the metabotropic glutamate receptor 1 (mGlu1), a G protein-coupled receptor involved in synaptic transmission and neuronal excitability. As a positive allosteric modulator, it binds to a site distinct from the glutamate binding site and enhances the receptor's response to glutamate. This allosteric modulation increases mGlu1 receptor activity without directly activating the receptor.
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| ln Vitro |
In vitro, Ro0711401 is a selective and orally active positive allosteric modulator of the mGlu1 receptor with an EC50 of 56 nM. Its activity is confirmed in cell-based assays measuring mGlu1 receptor-mediated calcium mobilization or downstream signaling. Its selectivity for mGlu1 over other mGlu receptors has been characterized.
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| ln Vivo |
Exercise performance improves with RO0711401 (10 mg/kg; subcutaneous injection; once) in a way that lasts at least six days [1]. Research has demonstrated that systemic injection of RO0711401 can enhance motor symptoms in mice with autoimmune encephalomyelitis (EAE) and decrease the frequency of spike-wave discharge in a rat model of absence epilepsy [1].
In vivo, Ro0711401 has oral activity. Its positive allosteric modulation of mGlu1 receptors suggests potential applications in neurological disorders involving glutamatergic signaling. However, specific in vivo efficacy data in animal models are limited. |
| Enzyme Assay |
Cell-free assays for Ro0711401 are not standard because it targets a receptor. Its binding to mGlu1 can be assessed using radioligand binding assays with membrane preparations from cells expressing mGlu1. Its positive allosteric modulation can be measured in functional assays using purified receptor or membrane preparations. Its molecular weight (360.29) and formula (C18H11F3N2O3) are confirmed by mass spectrometry.
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| Cell Assay |
Cellular assays for Ro0711401 are performed using cell lines expressing mGlu1 receptors. Cells are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of Ro0711401 in the presence of a submaximal concentration of glutamate. Calcium mobilization is measured, and the EC50 for potentiation of glutamate response is determined.
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| Animal Protocol |
Animal/Disease Models: Spinocerebellar Ataxia Type 1 (SCA1) Mice (30 weeks old) [1]
Doses: 10 mg/kg Route of Administration: subcutaneous injection; Primary Experimental Results: Results in motor performance in rotarod and paw print tests Long term improvement. In vivo animal experiments for Ro0711401 are not extensively documented. To study its effects on mGlu1 receptor function, animal models of pain, anxiety, or neurodegenerative diseases could be used. Animals would be administered Ro0711401 orally, and behavioral or physiological endpoints would be assessed. |
| ADME/Pharmacokinetics |
Ro0711401 has a molecular weight of 360.29 g/mol and a molecular formula of C18H11F3N2O3. It is a solid powder. It is soluble in DMSO at 100 mg/mL. It should be stored at -20°C for 3 years or 4°C for 2 years. Its chemical name is N-(4-(trifluoromethyl)oxazol-2-yl)-9H-xanthene-9-carboxamide.
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| Toxicity/Toxicokinetics |
The toxicological profile of Ro0711401 has not been extensively characterized. As a research compound, it is generally considered safe at the concentrations used in studies. No significant toxicity has been reported. Comprehensive toxicology studies are lacking. It is not an approved drug and is intended for research use only.
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| References |
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| Additional Infomation |
Ro0711401 is a selective and orally active positive allosteric modulator of the mGlu1 receptor with an EC50 of 56 nM. It is also known as Ro-0711401. It is a research compound for studying metabotropic glutamate receptor signaling in neurological disorders. It is not approved for clinical use.
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| Molecular Formula |
C18H11F3N2O3
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| Molecular Weight |
360.29
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| Exact Mass |
360.072
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| Elemental Analysis |
C, 60.01; H, 3.08; F, 15.82; N, 7.78; O, 13.32
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| CAS # |
714971-87-6
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| PubChem CID |
10338547
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.606
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| LogP |
3.21
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
508
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1=C([H])OC(=N1)N([H])C(C1([H])C2=C([H])C([H])=C([H])C([H])=C2OC2=C([H])C([H])=C([H])C([H])=C12)=O)(F)F
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| InChi Key |
GSGDLBUOSWGZER-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H11F3N2O3/c19-18(20,21)14-9-25-17(22-14)23-16(24)15-10-5-1-3-7-12(10)26-13-8-4-2-6-11(13)15/h1-9,15H,(H,22,23,24)
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| Chemical Name |
N-[4-(trifluoromethyl)-1,3-oxazol-2-yl]-9H-xanthene-9-carboxamide
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| Synonyms |
Ro 0711401; Ro-0711401; Ro0711401
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~277.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7755 mL | 13.8777 mL | 27.7554 mL | |
| 5 mM | 0.5551 mL | 2.7755 mL | 5.5511 mL | |
| 10 mM | 0.2776 mL | 1.3878 mL | 2.7755 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.
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