| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Cholecystokinin-B (CCK-B) receptor. LY262691 is a selective antagonist of the CCK-B receptor, a G protein-coupled receptor that binds cholecystokinin and gastrin. CCK-B receptors are expressed in the brain and gastrointestinal tract and are involved in anxiety, pain perception, and dopamine regulation. By blocking CCK-B receptors, LY262691 modulates midbrain dopamine neuron activity, which contributes to its antipsychotic properties.
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|---|---|
| ln Vitro |
LY262691 is a selective CCK-B antagonist that decreases midbrain dopamine unit activity. The compound reduces the number of spontaneously active A9 and A10 dopamine cells in the midbrain. Quantitative potency data such as IC50 or Ki values are not extensively reported in the available literature.
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| ln Vivo |
No specific in vivo efficacy data are reported for LY262691 in animal models in the available literature. The compound is characterized as a selective CCK-B antagonist with antipsychotic properties that decreases midbrain dopamine unit activity. Detailed pharmacokinetic parameters, dose-response relationships, and efficacy data in psychosis models are not extensively reported.
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| Enzyme Assay |
Representative protocol: For CCK-B receptor binding assays, membranes from cells expressing recombinant human CCK-B receptors or guinea pig brain membranes are incubated with test compound and a fixed concentration of a radiolabeled CCK-B antagonist such as [3H]-CCK-8 or [125I]-CCK-8 in assay buffer. Nonspecific binding is determined using unlabeled CCK-8. After incubation at 25 degrees Celsius for 60 to 120 minutes, samples are filtered over glass fiber filters and washed. Bound radioactivity is measured by liquid scintillation counting.
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| Cell Assay |
Representative protocol: For functional assays, cells expressing the CCK-B receptor are used to measure CCK-8-induced calcium mobilization or inositol phosphate production. Cells are loaded with a calcium-sensitive fluorescent dye, and changes in intracellular calcium are monitored using a fluorescence imaging plate reader upon addition of CCK-8 in the presence or absence of test compound. The ability of test compound to inhibit CCK-8-induced calcium flux is assessed.
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| Animal Protocol |
Representative protocol: For in vivo studies, rats are administered test compound intraperitoneally or orally at various doses. Midbrain dopamine neuron activity is measured using in vivo extracellular recording techniques. The number of spontaneously active A9 and A10 dopamine cells is quantified. Behavioral tests such as amphetamine-induced hyperlocomotion or conditioned avoidance response are used to assess antipsychotic-like activity.
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| References |
| Molecular Formula |
C22H18BRN3O2
|
|---|---|
| Molecular Weight |
436.31
|
| Exact Mass |
435.058
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| CAS # |
138932-35-1
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| PubChem CID |
132190
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.476g/cm3
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| Index of Refraction |
1.676
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| LogP |
5.139
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
552
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
BrC1C=CC(NC(N2NC(=O)C(C3C=CC=CC=3)C2C2C=CC=CC=2)=O)=CC=1
|
| InChi Key |
LMUQHXHWJWQXSD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18BrN3O2/c23-17-11-13-18(14-12-17)24-22(28)26-20(16-9-5-2-6-10-16)19(21(27)25-26)15-7-3-1-4-8-15/h1-14,19-20H,(H,24,28)(H,25,27)
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| Chemical Name |
N-(4-bromophenyl)-3-oxo-4,5-diphenylpyrazolidine-1-carboxamide
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| Synonyms |
LY-262691; LY 262691; LY262691
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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 | 2.2919 mL | 11.4597 mL | 22.9195 mL | |
| 5 mM | 0.4584 mL | 2.2919 mL | 4.5839 mL | |
| 10 mM | 0.2292 mL | 1.1460 mL | 2.2919 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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