Sograzepide
Based on 1 publication(s) in Google Scholar
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent, highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
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- Pureza: 98.04%
- No. CAS: 155488-25-8
- Fòrmula: C28H30N6O3
- Peso molecular:498.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Sograzepide
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Actividad biológica
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CCKBR |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 155488-25-8
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Appearance Solid
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Peso molecular 498.58
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Fòrmula C28H30N6O3
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CC(NC)=C1)N[C@H]2C(N(CC(C(C)(C)C)=O)C3=CC=CC=C3C(C4=NC=CC=C4)=N2)=O
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Synonyms
Netazepide; YF 476; YM-220
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Discovery of a β-arrestin-biased CCKBR agonist that blocks CCKBR-dependent long-term potentiation. [Abstract]2025 Dec 8;16(1):10938. PMID: 41360797
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (200.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Boyce M, et al. Effect of netazepide, a gastrin/CCK2 receptor antagonist, on gastric acid secretion and rabeprazole-induced hypergastrinaemia in healthy subjects. Br J Clin Pharmacol. 2015 May;79(5):744-55. [Content Brief]
[2]. Takinami Y, et al. YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo.Aliment Pharmacol Ther. 1997 Feb;11(1):113-20. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0057 mL | 10.0285 mL | 20.0570 mL | 50.1424 mL |
| 5 mM | 0.4011 mL | 2.0057 mL | 4.0114 mL | 10.0285 mL | |
| 10 mM | 0.2006 mL | 1.0028 mL | 2.0057 mL | 5.0142 mL | |
| 15 mM | 0.1337 mL | 0.6686 mL | 1.3371 mL | 3.3428 mL | |
| 20 mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.5071 mL | |
| 25 mM | 0.0802 mL | 0.4011 mL | 0.8023 mL | 2.0057 mL | |
| 30 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL | 1.6714 mL | |
| 40 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2536 mL | |
| 50 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 60 mM | 0.0334 mL | 0.1671 mL | 0.3343 mL | 0.8357 mL | |
| 80 mM | 0.0251 mL | 0.1254 mL | 0.2507 mL | 0.6268 mL | |
| 100 mM | 0.0201 mL | 0.1003 mL | 0.2006 mL | 0.5014 mL |
Sograzepide Related Classifications
HY-14850 Related Classifications
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