| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Basimglurant sulfate (RG7090; RO491752) is a potent, selective and orally bioavailable mGlu5 negative allosteric modulator with a Kd of 1.1 nM. It is being studied in a Phase 2 clinical trial to treat FXS and MDD. A promising new treatment for psychiatric conditions is basimglurant. Due to its advantageous drug-like characteristics, distinct molecular mechanism of action, and antidepressant-like qualities, basimglurant may also be able to treat significant MDD comorbidities like pain and anxiety, as well as daytime sleepiness, apathy, and lethargy.
| Targets |
mGlu5 Receptor ( Kd = 1.1 nM )
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|---|---|
| ln Vitro |
[3H]-basimglurant saturation analysis of recombinant human mGlu5 shows a single-phase saturation isotherm with a Kd of 1.1 nM. In competition binding experiments with human recombinant mGlu5, Basimglurant (RG7090) completely replaced [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quiescentine-induced Ca2+ mobilization with an IC50 of 7.0 nM and inhibits [3H]-inositol phosphate accumulation with an IC50 of 5.9 nM. Basimglurant (RG7090) shows similar potency in radioligand binding and functional assays of human and rodent mGlu5 receptor orthologues [1].
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| ln Vivo |
Basimglurant (RG7090) is a potent, selective and safe mGlu5 inhibitor with good oral bioavailability and long half-life supporting once-daily dosing, good brain penetration and high in vivo potency. It has antidepressant properties, confirmed by its functional magnetic imaging (fMRI) profile, as well as anxiolytic and antinociceptive properties [1]. It is currently in Phase II clinical studies for the treatment of depression and fragile X syndrome. Basimglurant dose-dependently increased drinking duration in the Vogel conflict drinking test. Total plasma exposure at effective doses of Basimglurant (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg) [2].
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| References |
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| Additional Infomation |
Basimglurant has been used in trials studying the diagnostic and treatment of Depression, Fragile X Syndrome, and Major Depressive Disorder.
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| Molecular Formula |
C18H13CLFN3
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|---|---|
| Molecular Weight |
325.76700
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| Exact Mass |
325.078
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| Elemental Analysis |
C, 66.36; H, 4.02; Cl, 10.88; F, 5.83; N, 12.90
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| CAS # |
802906-73-6
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| Related CAS # |
802906-73-6 (Sulfate); 1034442-21-1
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| PubChem CID |
11438771
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
526.6±60.0 °C at 760 mmHg
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| Flash Point |
272.3±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.604
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| LogP |
4.49
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
465
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(N2C(C)=C(C#CC3C=C(Cl)N=CC=3)N=C2C)=CC=1
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| Synonyms |
RO4917523;RG-7090; RG 7090; RO 4917523; RG7090; RO-4917523; Basimglurant
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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: ≥ 33.33 mg/mL (~102.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (7.67 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0697 mL | 15.3483 mL | 30.6965 mL | |
| 5 mM | 0.6139 mL | 3.0697 mL | 6.1393 mL | |
| 10 mM | 0.3070 mL | 1.5348 mL | 3.0697 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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