| Size | Price | Stock | Qty |
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| Targets |
Cholecystokinin-2 (CCK2/CCK-B) receptor. LY-288513 is a selective antagonist of the CCK2 receptor, a G protein-coupled receptor that binds cholecystokinin and gastrin. CCK2 receptors are expressed in the brain and gastrointestinal tract and are involved in anxiety, pain perception, and immune regulation. By blocking CCK2 receptors, LY-288513 inhibits CCK-8-induced signaling in immune cells.
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| ln Vitro |
The effects of CCK-8 on transcription factors unique to CD4+ T cell subsets are inhibited by LY288513 (10 nM; 2 days) [2].
LY-288513 is a selective CCK2 receptor antagonist. The compound inhibits CCK-8-induced effects on transcription factors unique to CD4+ T cell subsets at 10 nM. Quantitative potency data such as IC50 or Ki values are not extensively reported in the available literature. |
| ln Vivo |
In mice, LY288513 (3, 10 mg/kg intraperitoneal injection; 10, 30 mg/kg oral) has effects similar to those of anxiolytics [3]. At the largest dosage studied, LY288513 (1000 mg/kg, oral) only causes mild hypothermia, amplifies the effects of CNS depressants, and is only mildly sedative [3].
No specific in vivo efficacy data are reported for LY-288513 in animal models in the available literature. The compound is characterized primarily for its in vitro activity as a CCK2 receptor antagonist and its effects on immune cell signaling. No animal efficacy, pharmacokinetic, or toxicological data are available in the current literature. |
| Enzyme Assay |
Representative protocol: For CCK2 receptor binding assays, membranes from cells expressing recombinant human CCK2 receptors or guinea pig brain membranes are incubated with test compound and a fixed concentration of a radiolabeled CCK2 antagonist such as [3H]-CCK-8 or [125I]-CCK-8 in assay buffer. Nonspecific binding is determined using unlabeled CCK-8. After incubation, samples are filtered and bound radioactivity is measured.
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| Cell Assay |
RT-PCR[2]
Cell Types: CD4+ T cells Tested Concentrations: 10 nM Incubation Duration: 2 days Experimental Results: Effect of inhibition of CCK-8 on CD4+ T cell subset-specific transcription factors. Representative protocol: For cell-based assays, CD4+ T cells are isolated and cultured, then treated with test compound in the presence or absence of CCK-8. Activation of transcription factors unique to CD4+ T cell subsets is measured using reporter gene assays or EMSA. Cytokine production is measured by ELISA. Cell viability is assessed using MTT or resazurin assays. |
| Animal Protocol |
Animal/Disease Models: Male CD-1 mice [3]
Doses: 3, 10 mg/kg; 10, 30 mg/kg Route of Administration: intraperitoneal (ip) injection; po Experimental Results: demonstrated anxiolytic-like effects in the elevated plus maze. Representative protocol: For in vivo studies, a general approach for evaluating CCK2 receptor antagonists involves using rodent models of anxiety (elevated plus maze, light-dark box) and immune function. Test compound is administered intraperitoneally or orally at various doses, and behavioral or immune parameters are measured. For immune studies, CD4+ T cell responses are assessed by flow cytometry and cytokine profiling. |
| References |
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| Additional Infomation |
(4S,5R)-N-(4-bromophenyl)-3-oxo-4,5-diphenyl-1-pyrazolidinecarboxamide is a stilbene compound. See also: ... View more ...
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| Molecular Formula |
C22H18BRN3O2
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|---|---|
| Molecular Weight |
436.31
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| Exact Mass |
435.058
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| CAS # |
147523-65-7
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| Related CAS # |
LY262691; 138932-35-1
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| PubChem CID |
2802894
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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 |
5.192
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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 |
3
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| Heavy Atom Count |
28
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| Complexity |
552
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| Defined Atom Stereocenter Count |
2
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| SMILES |
BrC1C=CC(=CC=1)N([H])C(N1[C@@H](C2C=CC=CC=2)[C@H](C2C=CC=CC=2)C(N1[H])=O)=O
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| InChi Key |
LMUQHXHWJWQXSD-PMACEKPBSA-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)/t19-,20-/m0/s1
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| Chemical Name |
(4S,5R)-N-(4-bromophenyl)-3-oxo-4,5-diphenylpyrazolidine-1-carboxamide
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| Synonyms |
LY288513 LY 288513 LY-288513
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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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