| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
The primary target of SCH-50911 is the GABA-B receptor, a G protein-coupled receptor that mediates slow inhibitory neurotransmission. It acts as a competitive antagonist at the orthosteric binding site. By blocking GABA-B receptors, it prevents the inhibitory effects of GABA and baclofen, leading to increased neuronal excitability. Its selectivity for GABA-B over GABA-A is high, making it a valuable tool.
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| ln Vitro |
In vitro, SCH-50911 demonstrates potent antagonism of GABA-B receptors. It has an IC₅₀ in the nanomolar range for inhibiting GABA-stimulated [³⁵S]GTPγS binding. It reverses the effects of the GABA-B agonist baclofen in electrophysiological recordings from hippocampal neurons. The compound's activity is characterized in radioligand binding and functional assays, confirming its role as a competitive antagonist.
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| ln Vivo |
In vivo, SCH-50911 has been shown to produce pro-cognitive effects and to modulate anxiety-like behaviors. It can reverse baclofen-induced hypothermia and memory deficits in rodents. It is used to study the involvement of GABA-B receptors in learning and memory, as well as in addiction models where it can reduce the rewarding effects of drugs of abuse. Its effects are dose-dependent and route-dependent.
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| Enzyme Assay |
In vitro receptor binding studies for SCH-50911 measure its affinity for the GABA-B receptor. Radioligand competition assays use [³H]CGP54626 or [¹²⁵I]CGP71872 as the labeled ligand. Membrane preparations from rat brain or cells expressing recombinant GABA-B receptors are used. The compound's Ki value is determined from competition curves. Selectivity over GABA-A is confirmed by lack of binding at high concentrations.
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| Cell Assay |
In vitro cell-based functional assays for SCH-50911 evaluate its ability to block GABA-B receptor signaling. Cells expressing GABA-B receptors are stimulated with baclofen, and downstream signaling such as inhibition of cAMP accumulation is measured. The compound is added at various concentrations to determine the IC₅₀ for reversing the baclofen effect. These assays are performed in standard cell culture conditions.
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| Animal Protocol |
In vivo animal studies for SCH-50911 typically involve rodents. The compound is administered intraperitoneally or orally. Behavioral tests include the Morris water maze for spatial memory, elevated plus maze for anxiety, and conditioned place preference for addiction. Physiological parameters like body temperature are also monitored. The compound's effects are compared to baclofen and other GABA-B modulators.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of SCH-50911 include good brain penetration and oral bioavailability. Its molecular weight is 283.19 g/mol. The compound is soluble in DMSO. Storage conditions are typically at -20°C, protected from moisture. Detailed PK parameters such as half-life and Cmax are available from published studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of SCH-50911 is not extensively reported, but as a research compound, it is intended for non-human use. At higher doses, it may cause convulsions or other excitatory effects due to GABA-B blockade. Standard safety precautions for handling neuroactive compounds should be followed.
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| References | |
| Additional Infomation |
Additional information: SCH-50911 is also known as (R,S)-3-amino-2-(2,6-dichlorophenyl)-1,1-difluoropropanol. It is a racemic mixture, with the (S)-enantiomer being more potent. It is used extensively in neuroscience research. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C8H15NO3
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|---|---|
| Molecular Weight |
173.209602594376
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| Exact Mass |
173.105
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| CAS # |
733717-87-8
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| Related CAS # |
SCH 50911 hydrochloride;160415-07-6
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| PubChem CID |
5311429
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| Appearance |
White to off-white solid powder
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| LogP |
0.556
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
179
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1(CO[C@H](CN1)CC(=O)O)C
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| InChi Key |
SEYCKMQSPUVYEF-LURJTMIESA-N
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| InChi Code |
InChI=1S/C8H15NO3/c1-8(2)5-12-6(4-9-8)3-7(10)11/h6,9H,3-5H2,1-2H3,(H,10,11)/t6-/m0/s1
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| Chemical Name |
2-[(2S)-5,5-dimethylmorpholin-2-yl]acetic 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 5.7733 mL | 28.8667 mL | 57.7334 mL | |
| 5 mM | 1.1547 mL | 5.7733 mL | 11.5467 mL | |
| 10 mM | 0.5773 mL | 2.8867 mL | 5.7733 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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