YM022
Based on 2 publication(s) in Google Scholar
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
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- Reinheit: 99.87%
- CAS. Nr.: 145084-28-2
- Formel: C32H28N4O3
- Molecular Weight:516.59
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) YM022
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CCR2 68 pM (Ki) |
CCR1 63 nM (Ki) |
In Vitro
YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC50 value for [3H]devazepide binding of 136 nM[1].
YM022 inhibits the binding of [125I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC50 value for [125I]CCK-8 binding of 0.73 nM[1].
Selectivity [ratio of (IC50 for gastrin/CCK-B receptor)/(IC50for CCK-A receptor)] of YM022 is 186[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
YM022 (subcutaneous injection; 300 μmol/kg; single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24 h after dosage). Maximum enzyme inhibition is achieved at a dose of 300 μmol/kg for YM022 and the inhibition of HDC lasts for 4 weeks. At sacrifice, drug residues can be seen at the injection site for as long as 4 (YM022) weeks after injection in rat[3].
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat[3]
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Dosage:300 μmol/kg
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Administration:Subcutaneous injection; 300 μmol/kg; single dose
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Result:Suppressed the ECL cell activity for at least 4 as manifested in greatly reduced HDC activity, greatly elevated serum gastrin level.
Chemical Information
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CAS. Nr. 145084-28-2
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Appearance Solid
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Molecular Weight 516.59
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Formel C32H28N4O3
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(CC(C3=CC=CC=C3C)=O)C4=CC=CC=C4C(C5=CC=CC=C5)=N2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Peptides
Cholecystokinin regulates atrial natriuretic peptide secretion through activation of NOX4-Sirt1-LEF1 signaling in beating rat hypoxic atria. [Abstract]2024 Nov:181:171299. PMID: 39326462 -
Oxid Med Cell Longev
Cholecystokinin Octapeptide Promotes ANP Secretion through Activation of NOX4-PGC-1 α-PPAR α/PPAR γ Signaling in Isolated Beating Rat Atria. [Abstract]2022 Jun 20;2022:5905374. PMID: 35770043
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (193.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Nishida A, et al. Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.J Pharmacol Exp Ther. 1994 May;269(2):725-31. [Content Brief]
[2]. Kitano M, et al. Long-lasting cholecystokinin(2) receptor blockade after a single subcutaneous injection of YF476 or YM022.Br J Pharmacol. 2000 Jun;130(3):699-705. [Content Brief]
[3]. Beinborn M, et al. Small synthetic ligands of the cholecystokinin-B/gastrin receptor can mimic the function of endogenous peptide hormones.Yale J Biol Med. 1998 May-Aug;71(3-4):337-46. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9358 mL | 9.6789 mL | 19.3577 mL | 48.3943 mL |
| 5 mM | 0.3872 mL | 1.9358 mL | 3.8715 mL | 9.6789 mL | |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9358 mL | 4.8394 mL | |
| 15 mM | 0.1291 mL | 0.6453 mL | 1.2905 mL | 3.2263 mL | |
| 20 mM | 0.0968 mL | 0.4839 mL | 0.9679 mL | 2.4197 mL | |
| 25 mM | 0.0774 mL | 0.3872 mL | 0.7743 mL | 1.9358 mL | |
| 30 mM | 0.0645 mL | 0.3226 mL | 0.6453 mL | 1.6131 mL | |
| 40 mM | 0.0484 mL | 0.2420 mL | 0.4839 mL | 1.2099 mL | |
| 50 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9679 mL | |
| 60 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8066 mL | |
| 80 mM | 0.0242 mL | 0.1210 mL | 0.2420 mL | 0.6049 mL | |
| 100 mM | 0.0194 mL | 0.0968 mL | 0.1936 mL | 0.4839 mL |
YM022 Related Classifications
HY-103355 Related Classifications
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