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| Targets |
BNC375 targets α7 nicotinic acetylcholine receptors (α7 nAChRs). These receptors are ligand-gated ion channels involved in cognitive function, memory, and neuropsychiatric processes. BNC375 acts as a type I positive allosteric modulator (PAM), meaning it enhances the receptor's response to acetylcholine without directly activating the receptor itself. It has an EC50 of 1.9 μM for α7 nAChR modulation. The compound shows good selectivity for α7 nAChRs.
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| ln Vitro |
Without changing the rate of fast receptor desensitization, BNC375 dramatically increases acetylcholine signaling [1].
In vitro, BNC375 potentiates α7 nAChR activity with an EC50 of 1.9 μM. As a type I PAM, it enhances the receptor's response to orthosteric agonists without directly activating the receptor. The compound exhibits good CNS drug-like properties. These properties make BNC375 a valuable tool for studying α7 nAChR biology and evaluating PAMs as therapeutic strategies for cognitive disorders. |
| ln Vivo |
In the mouse T-maze experiment, BNC375 (0.003–10.0 mg/kg, oral) totally reverses the harm that 1.0 mg/kg scopolamine causes (MED = 0.03 mg/kg). BNC375 has a plasma half-life (t1/2) of 1.2 hours [1].
In vivo, BNC375 is orally available and exhibits a plasma half-life of 1.2 hours. It has been studied for potential therapeutic benefits in Alzheimer's disease, schizophrenia, and other cognitive disorders. The compound shows good CNS drug-like properties and clinical candidate potential. Specific animal model data and dosing regimens are available in the primary literature. |
| Enzyme Assay |
Not specifically documented for BNC375. For α7 nAChR positive allosteric modulators, cell-free binding assays typically measure the binding of radiolabeled orthosteric ligands (e.g., α-bungarotoxin) to α7 nAChR preparations. The allosteric modulation can be assessed using electrophysiological techniques with isolated receptors or membrane preparations. EC50 values are determined from concentration-response curves.
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| Cell Assay |
In vitro cell-based assays for BNC375 include electrophysiological recordings (patch-clamp) in cells expressing α7 nAChRs to assess modulation of receptor function. Calcium flux assays using fluorescent calcium indicators can measure receptor activation and potentiation. The compound is typically tested at concentrations around its EC50 of 1.9 μM. Selectivity profiling against other nicotinic receptor subtypes may be performed.
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| Animal Protocol |
In vivo studies with BNC375 are conducted in animal models of cognitive disorders such as Alzheimer's disease and schizophrenia. The compound is administered orally due to its oral bioavailability. Endpoints include cognitive performance assessments, receptor occupancy studies, and evaluation of CNS exposure. Dosing regimens are detailed in the primary literature.
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| ADME/Pharmacokinetics |
BNC375 is orally available and has a plasma half-life of 1.2 hours. As a small molecule with molecular weight 394.92 and formula C19H23ClN2O3S, it exhibits good CNS drug-like properties. The compound appears as a solid. Detailed PK parameters such as Cmax and AUC are available in the primary literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BNC375 are not provided in the available literature. As a research compound, it is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. The compound is supplied for research purposes only.
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| References | |
| Additional Infomation |
α7 Nicotine acetylcholine receptor positive allosteric modulator
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. The molecular formula is C19H23ClN2O3S with a molecular weight of 394.92. The compound exhibits good CNS drug-like properties and clinical candidate potential. It is used in neuroscience research for cognitive disorders. |
| Molecular Formula |
C19H23CLN2O3S
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|---|---|
| Molecular Weight |
394.915522813797
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| Exact Mass |
394.1118
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| CAS # |
1557240-80-8
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| PubChem CID |
118160666
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
584
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1C=CC(=C(C=1)NC[C@@H]1[C@@H](C2C=CC(=CC=2)S(N)(=O)=O)C1(C)C)OC
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| InChi Key |
LWWDCTBUJUEFDE-CRAIPNDOSA-N
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| InChi Code |
InChI=1S/C19H23ClN2O3S/c1-19(2)15(11-22-16-10-13(20)6-9-17(16)25-3)18(19)12-4-7-14(8-5-12)26(21,23)24/h4-10,15,18,22H,11H2,1-3H3,(H2,21,23,24)/t15-,18-/m1/s1
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| Chemical Name |
4-[(1R,3R)-3-[(5-chloro-2-methoxyanilino)methyl]-2,2-dimethylcyclopropyl]benzenesulfonamide
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| Synonyms |
BNC 375; BNC-375; BNC375
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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 : ~83.33 mg/mL (~211.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.27 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 20.8 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: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (5.27 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 | 2.5322 mL | 12.6608 mL | 25.3216 mL | |
| 5 mM | 0.5064 mL | 2.5322 mL | 5.0643 mL | |
| 10 mM | 0.2532 mL | 1.2661 mL | 2.5322 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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