| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| Targets |
TCS-46b targets the NMDA receptor, specifically the NR1A/2B subtype. It is a subtype-selective NR1A/2B NMDA receptor antagonist with an IC50 of 5.3 nM. It exhibits high selectivity for NR1A/2B over NR1A/2A (IC50 = 35,000 nM) and NR1A/2C (IC50 > 100,000 nM). By selectively blocking NR2B-containing NMDA receptors, TCS-46b modulates glutamatergic neurotransmission.
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| ln Vitro |
In vitro, TCS-46b is a potent, selective NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM. It exhibits high selectivity for NR1A/2B over other NMDA receptor subtypes. These in vitro properties make TCS-46b a valuable tool for studying NR2B-containing NMDA receptor function and its role in neurological and psychiatric disorders.
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| ln Vivo |
TCS 46b (Compound 46b; 10 and 30 mg/kg; po or ip; once) potentiates the effects of levodopa in 6-OHDA lesions [1].
In vivo, TCS-46b is an orally active NMDA NR1A/2B receptor antagonist. Its selectivity for NR2B-containing NMDA receptors suggests potential for treating neurological and psychiatric disorders without the side effects associated with non-selective NMDA receptor antagonists. However, detailed in vivo efficacy data are limited in publicly available sources. |
| Enzyme Assay |
The in vitro receptor binding assay for TCS-46b involves measuring its binding affinity to NMDA receptor subtypes. The compound is incubated with membranes expressing NR1A/2B, NR1A/2A, or NR1A/2C receptors in the presence of a radiolabeled ligand (e.g., [3H]MK-801 or [3H]ifenprodil). Binding affinity (IC50 or Ki) is determined using competition binding assays. Functional antagonism can be assessed by measuring NMDA-induced calcium influx or electrophysiological responses in cells expressing the receptor subtypes.
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| Cell Assay |
The in vitro cell-based assay for TCS-46b involves culturing cells expressing NMDA receptor subtypes (e.g., NR1A/2B, NR1A/2A, NR1A/2C) and treating them with the compound to assess effects on receptor function. Cells are treated with TCS-46b at various concentrations in the presence of NMDA and glycine. Receptor activity is measured by assessing calcium influx using fluorescent calcium indicators (e.g., Fluo-4) or by measuring downstream signaling. Selectivity for NR2B-containing receptors is confirmed by comparing IC50 values across subtypes. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
Animal/Disease Models: Sprague−Dawley rat, 6-hydroxydopamine injury (6-OHDA) rat model [1]
Doses: 10 and 30 mg/kg Route of Administration: Oral or intraperitoneal (ip) injection once Experimental Results: L was shown in this model -The effect of DOPA is Dramatically enhanced. In vivo animal studies for TCS-46b have not been extensively reported. If conducted, such studies might involve mouse or rat models of neurological or psychiatric disorders, such as pain, depression, or Parkinson's disease. TCS-46b would be administered orally at various doses, and behavioral, biochemical, and histological endpoints would be assessed. Standard protocols for these models would be employed. No specific data are available. |
| ADME/Pharmacokinetics |
TCS-46b is an orally active small molecule with favorable pharmacokinetic properties. It has a molecular weight of 345.44 and a molecular formula of C22H23N3O. The compound is soluble in DMSO and can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources but are expected to be characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of TCS-46b has not been systematically evaluated. As a selective NR2B-containing NMDA receptor antagonist, its primary safety concerns would relate to on-target effects on glutamatergic neurotransmission. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References | |
| Additional Infomation |
TCS-46b is a research compound and has not been approved for clinical use. It is a potent, selective, and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM and high selectivity over NR1A/2A and NR1A/2C. TCS-46b is a valuable tool for studying NR2B-containing NMDA receptor function and its role in neurological and psychiatric disorders.
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| Molecular Formula |
C22H23N3O
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| Molecular Weight |
345.446
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| Exact Mass |
345.184
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| Elemental Analysis |
C, 76.49; H, 6.71; N, 12.16; O, 4.63
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| CAS # |
302799-86-6
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| PubChem CID |
9863010
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
548
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JJEXWPHPFZLTCU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23N3O/c26-22-23-20-9-8-18(16-21(20)24-22)7-4-12-25-13-10-19(11-14-25)15-17-5-2-1-3-6-17/h1-3,5-6,8-9,16,19H,10-15H2,(H2,23,24,26)
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| Chemical Name |
5-(3-(4-benzylpiperidin-1-yl)prop-1-yn-1-yl)-1,3-dihydro-2H-benzo[d]imidazol-2-one
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| Synonyms |
TCS 46b; TCS-46b; TCS46b;
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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 (~289.49 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 | 2.8948 mL | 14.4739 mL | 28.9477 mL | |
| 5 mM | 0.5790 mL | 2.8948 mL | 5.7895 mL | |
| 10 mM | 0.2895 mL | 1.4474 mL | 2.8948 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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