| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
CCK-B Receptor Antagonist 1 targets the cholecystokinin B (CCK-B) receptor, a G protein-coupled receptor that mediates the effects of cholecystokinin. CCK-B receptors are involved in the regulation of gastric acid secretion, appetite, and anxiety. By blocking CCK-B receptors, the compound may reduce gastric acid secretion.
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| ln Vitro |
(Rac)-Sograzepide is an antagonist of the CCK-B receptor that may lessen the production of gastric acid [1].
CCK-B Receptor Antagonist 1 demonstrates in vitro antagonism of the CCK-B receptor. The compound shows potential for reducing gastric acid secretion. As a CCK-B receptor antagonist, it is used as a research tool to study the role of CCK-B receptors in gastrointestinal function and other physiological processes. |
| ln Vivo |
In vivo, CCK-B Receptor Antagonist 1 is used as a research tool to study CCK-B receptor function and its role in gastric acid secretion and other physiological processes. The compound has the potential to reduce gastric acid secretion in vivo. Further in vivo studies would be required to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro receptor binding assays for CCK-B Receptor Antagonist 1 typically employ membrane preparations from cells expressing human or rodent CCK-B receptors. Radioligand binding assays using ¹2⁵I-labeled CCK-8 or other appropriate radioligands are performed to determine binding affinity. Competition binding experiments are conducted with varying concentrations of the antagonist.
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| Cell Assay |
In vitro cellular assays for CCK-B Receptor Antagonist 1 involve treating cells expressing CCK-B receptors with varying concentrations of the compound (typically 0.001-100 microM range) prior to or concurrently with CCK-8 stimulation. Readouts include measurement of intracellular calcium mobilization (CCK-B is Gq-coupled), assessment of downstream signaling, and evaluation of receptor internalization.
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| Animal Protocol |
In vivo animal studies for CCK-B Receptor Antagonist 1 typically employ rodent models of gastric acid secretion. Animals are administered the compound via appropriate routes at various doses. Endpoints include measurement of gastric acid output, assessment of gastric pH, and evaluation of gastrointestinal function.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CCK-B Receptor Antagonist 1 are characteristic of small molecule receptor antagonists. With a molecular weight of 498.58, the compound is a small molecule. PK parameters including half-life, Cmax, Tmax, and AUC would be determined via LC-MS/MS analysis following administration in appropriate animal models.
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| Toxicity/Toxicokinetics |
CCK-B Receptor Antagonist 1 is a research-grade compound for laboratory use only. As with all research chemicals, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. The compound is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
CCK-B Receptor Antagonist 1 (CAS# 168161-71-5) is a CCK-B receptor antagonist with the potential to reduce gastric acid secretion. It is also known as (Rac)-Sograzepide or (Rac)-Netazepide. The compound is not approved for clinical use and is for research purposes only.
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| Molecular Formula |
C28H30N6O3
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|---|---|
| Molecular Weight |
498.5762
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| Exact Mass |
498.237
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| CAS # |
168161-71-5
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| Related CAS # |
Sograzepide;155488-25-8
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| PubChem CID |
21842392
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
869
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC=CC(NC)=C1)NC2C(N(CC(C(C)(C)C)=O)C3=CC=CC=C3C(C4=NC=CC=C4)=N2)=O
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| InChi Key |
YDZYKNJZCVIKPP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H30N6O3/c1-28(2,3)23(35)17-34-22-14-6-5-12-20(22)24(21-13-7-8-15-30-21)32-25(26(34)36)33-27(37)31-19-11-9-10-18(16-19)29-4/h5-16,25,29H,17H2,1-4H3,(H2,31,33,37)
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| Chemical Name |
1-[1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl]-3-[3-(methylamino)phenyl]urea
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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 : ~125 mg/mL (~250.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0057 mL | 10.0285 mL | 20.0570 mL | |
| 5 mM | 0.4011 mL | 2.0057 mL | 4.0114 mL | |
| 10 mM | 0.2006 mL | 1.0028 mL | 2.0057 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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