| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
GV150013 selectively targets the cholecystokinin-2 (CCK2) receptor, a G protein-coupled receptor involved in various physiological processes, including anxiety, pain perception, and sleep regulation. By acting as an antagonist, it blocks the binding of the endogenous ligand, cholecystokinin, to this receptor.
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| ln Vitro |
In vitro studies confirm the high affinity and selectivity of GV150013 for the CCK-B receptor. It acts as a potent antagonist, effectively blocking CCK-induced signaling in cell-based assays. Its selectivity over other related receptors makes it a valuable tool for studying CCK-B receptor function.
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| ln Vivo |
GV-150013 on REM sleep and REM sleep in aged mice (0.5 - 60 μg/kg, non-intravenous, in one dosage increment) [1].
In vivo, GV150013 (0.5 - 60 μg/kg, ip, Once) has been shown to increase both REM sleep and non-REM sleep in aged rat models. The duration of REM sleep and non-REM sleep was significantly longer than that of the control group. This indicates a sleep-promoting effect, particularly in aged subjects. |
| Enzyme Assay |
In vitro binding assays are used to determine the affinity and selectivity of GV150013 for the CCK-B receptor. These assays typically involve competition binding experiments using radiolabeled ligands and membrane preparations from cells expressing the receptor.
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| Cell Assay |
In vitro cell-based functional assays measure the antagonist activity of GV150013. Cells expressing the CCK-B receptor are stimulated with a CCK agonist, and the downstream signaling (e.g., calcium mobilization) is measured in the presence and absence of the compound. A reduction in signaling indicates antagonist activity.
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| Animal Protocol |
Animal/Disease Models: Aged rats [2].
Doses: 0.5μg/kg, 5μg/kg, 60μg/kg Route of Administration: intraperitoneal (ip) injection, once. Experimental Results: The duration of REM sleep and non-REM sleep was longer than the control. The in vivo activity of GV150013 is evaluated in rodent models, particularly aged rats. The compound is administered via intraperitoneal (ip) injection. Sleep patterns are monitored using electroencephalography (EEG) and electromyography (EMG) to measure changes in REM and non-REM sleep duration. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GV150013 are not extensively detailed in the literature. As a small molecule (MW 534.65) with activity via intraperitoneal injection, it is likely to have moderate bioavailability. Its ability to cross the blood-brain barrier is essential for its central nervous system effects on sleep.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for GV150013 is not available in the standard research literature. As a research compound, it is not intended for human use. Preclinical safety studies would be required to evaluate its toxicity profile for any potential therapeutic development.
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| References |
[1]. Crespi F. Cholecystokinin-B (CCK-B) receptor antagonists improve "aged" sleep: a new class of sleep modulators? Methods Find Exp Clin Pharmacol. 1999 Jan-Feb;21(1):31-8.
[2]. F.Crespi, et al. Influence of cholecystokinin-B (CCK-B) receptor antagonists on rat electroencephalography (EEG): A new class of sleep modulators? Gaviraghi. Dept of Pharmacology GlaxoWellcome S.p.A., Medicine Research Centre, via A. Fleming, 4, 37135 Verona, Italy |
| Additional Infomation |
GV 150013X is a benzodiazepine drug.
GV150013 is a research tool used to study the role of the CCK-B receptor in sleep regulation. It has not been developed as a therapeutic drug and is not approved for clinical use. Its ability to improve sleep in aged rats suggests a potential role for CCK-B antagonists in treating age-related sleep disturbances. |
| Molecular Formula |
C33H34N4O3
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|---|---|
| Molecular Weight |
534.66
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| Exact Mass |
534.263
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| CAS # |
167355-22-8
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| PubChem CID |
5311147
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.34±0.1 g/cm3(Predicted)
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| Boiling Point |
792.3±60.0 °C(Predicted)
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| LogP |
5.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
40
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| Complexity |
930
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C(NC(NC2C(=O)N(C3=CC=CC=C3)C3=CC=CC=C3N(CC34CC5CC(C3)CC(C5)C4)C2=O)=O)C=C1
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| InChi Key |
RZERRLOTRSJIAW-NEPGVILWSA-N
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| InChi Code |
InChI=1S/C33H34N4O3/c38-30-29(35-32(40)34-25-9-3-1-4-10-25)31(39)37(26-11-5-2-6-12-26)28-14-8-7-13-27(28)36(30)21-33-18-22-15-23(19-33)17-24(16-22)20-33/h1-14,22-24,29H,15-21H2,(H2,34,35,40)/t22?,23?,24?,29-,33?/m1/s1
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| Chemical Name |
1-[(3R)-1-(1-adamantylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-3-yl]-3-phenylurea
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| Synonyms |
GV-150013; GV 150013; GV150013
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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 | 1.8703 mL | 9.3517 mL | 18.7035 mL | |
| 5 mM | 0.3741 mL | 1.8703 mL | 3.7407 mL | |
| 10 mM | 0.1870 mL | 0.9352 mL | 1.8703 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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