| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
BINA targets the metabotropic glutamate receptor subtype 2 (mGluR2), a G protein-coupled receptor that modulates synaptic transmission. BINA is a selective positive allosteric modulator (PAM) of mGluR2, enhancing the receptor's response to glutamate without directly activating the receptor. By potentiating mGluR2 signaling, BINA reduces glutamatergic neurotransmission, which can have anxiolytic and antipsychotic effects. The compound's selectivity for mGluR2 over other mGluR subtypes makes it a valuable tool for studying mGluR2 function.
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| ln Vitro |
In the presence or absence of 5 μM glutamate, biphenylindane A (BINA) is active on the glutamate-induced scintillation proximity assay [3H]IP1 hydrolysis of WT mGluR2 (EC50=1.57 μM) [1].
In vitro, BINA is a selective positive allosteric modulator of mGluR2. It enhances the response of mGluR2 to glutamate in receptor binding and functional assays. In cell-based assays, BINA treatment results in potentiated mGluR2-mediated signaling, such as increased inhibition of cAMP accumulation or activation of G protein-coupled inward rectifying potassium (GIRK) channels. The compound's selectivity for mGluR2 over other mGluR subtypes is confirmed using selectivity profiling. BINA's allosteric modulation of mGluR2 makes it a valuable tool for studying mGluR2 function. |
| ln Vivo |
In vivo, BINA has been studied for its potential in the treatment of psychiatric disorders. As a positive allosteric modulator of mGluR2, BINA can reduce glutamatergic neurotransmission and produce anxiolytic and antipsychotic effects. The compound has been evaluated in animal models of anxiety, schizophrenia, and depression. BINA's effects on behavior and neural function are assessed using various behavioral tests and electrophysiological recordings. Comprehensive in vivo studies are ongoing.
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| Enzyme Assay |
In vitro receptor binding assays for BINA involve measuring its binding to the metabotropic glutamate receptor subtype 2 (mGluR2). The receptor is incubated with a radiolabeled ligand and varying concentrations of BINA. The compound's allosteric modulation is assessed by measuring the enhancement of agonist binding in the presence of BINA. Functional assays, such as measuring inhibition of cAMP accumulation or calcium mobilization, are used to confirm the compound's positive allosteric modulation. These assays confirm the compound's mechanism of action.
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| Cell Assay |
In vitro cell-based assays for BINA evaluate its effects on mGluR2-mediated signaling. Cells expressing mGluR2 are cultured and treated with BINA in the presence or absence of glutamate. The compound's enhancement of mGluR2-mediated signaling is assessed by measuring downstream effects such as inhibition of cAMP accumulation or activation of GIRK channels. These assays confirm the compound's functional activity as a positive allosteric modulator of mGluR2.
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| Animal Protocol |
In vivo animal experiments for BINA have been conducted in models of psychiatric disorders. Animals are treated with BINA, and behavioral effects are assessed using tests such as the elevated plus maze (for anxiety), prepulse inhibition (for schizophrenia), and forced swim test (for depression). Electrophysiological recordings are used to assess the compound's effects on neural activity. Pharmacokinetic studies are conducted to determine the compound's half-life, clearance, and tissue distribution. Comprehensive in vivo studies are ongoing.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for BINA are limited. The compound has a molecular weight of 410.41 g/mol. It is soluble in DMSO. The compound's metabolic stability, half-life, and bioavailability have not been fully characterized. Comprehensive ADME studies are needed to fully characterize the pharmacokinetic profile of BINA.
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| Toxicity/Toxicokinetics |
The toxicity profile of BINA has not been extensively characterized. In laboratory settings, BINA should be handled as a hazardous chemical. Appropriate personal protective equipment should be used when handling the compound. The compound is for research use only and is not intended for human or veterinary use. Comprehensive toxicological studies are needed to fully characterize the safety profile of BINA.
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| References | |
| Additional Infomation |
Biphenyl indanone a is a member of the biphenyl class of compounds.
BINA is a selective positive allosteric modulator of the metabotropic glutamate receptor subtype 2 (mGluR2). It has a molecular formula of C₁₈H₁₇F₃N₄O₂S and a molecular weight of 410.41 g/mol. BINA enhances the response of mGluR2 to glutamate, potentiating mGluR2-mediated signaling. The compound has been studied for its potential in the treatment of psychiatric disorders, including anxiety, schizophrenia, and depression. BINA is a valuable research tool for studying mGluR2 function. |
| Molecular Formula |
C30H30O4
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|---|---|
| Molecular Weight |
454.5568
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| Exact Mass |
454.214
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| CAS # |
866823-73-6
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| PubChem CID |
9868580
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
676.9±55.0 °C at 760 mmHg
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| Flash Point |
225.8±25.0 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.627
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| LogP |
8.27
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
719
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KMKBEESNZAPKMP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H30O4/c1-18-19(2)28-25(15-26(29(28)31)22-7-3-4-8-22)16-27(18)34-17-20-6-5-9-24(14-20)21-10-12-23(13-11-21)30(32)33/h5-6,9-14,16,22,26H,3-4,7-8,15,17H2,1-2H3,(H,32,33)
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| Chemical Name |
4-[3-[(2-cyclopentyl-6,7-dimethyl-1-oxo-2,3-dihydroinden-5-yl)oxymethyl]phenyl]benzoic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~219.99 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1999 mL | 10.9996 mL | 21.9993 mL | |
| 5 mM | 0.4400 mL | 2.1999 mL | 4.3999 mL | |
| 10 mM | 0.2200 mL | 1.1000 mL | 2.1999 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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