MK-0557
Based on 1 publication(s) in Google Scholar
MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.93%
- CAS 番号: 328232-95-7
- 分子式: C22H19FN4O3
- 分子量:406.41
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-107725
BIBO3304NPY Y1 Receptor Antagonist -
HY-107734
L 152804NPY Y5 Receptor Antagonist -
HY-107735
CYM 9484NPYY2 Receptor Antagonist -
HY-100717
HT-2157Gal3 Antagonist -
HY-101986
BIIE-0246NPY2R Antagonist -
HY-14423
VelneperitNeuropeptide Y Receptor Antagonist -
HY-14450
JNJ-31020028Y2 Receptor Antagonist -
HY-107723
CGP71683 hydrochlorideNeuropeptide Receptor Antagonist -
HY-P0198
Neuropeptide Y (human,rat,mouse)Active Compound -
HY-100717R
HT-2157 (Standard)Gal3 Antagonist -
HY-107733
NTNCB hydrochlorideNPY Y5 Receptor Antagonist -
HY-107382
RF9Neuropeptide Y Receptor Antagonist
MedChemExpress（MCE）の使用を引用している文献 MK-0557
MoreNeuropeptide Y Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
|
NPY Y5 receptor |
体外実験
Neuropeptide Y (NPY) is a potent orexigenic neuropeptide, and antagonism of NPY Y1 and NPY Y5 receptors (NPYxR) is considered a potentially important anti-obesity drug target. MK-0557 has a Ki=1.3 nM at the human NPY5R, with similar affinities at rhesus, mouse, and rat NPY5R. MK-0557 has no significant binding to the human NPY1R, NPY2R, NPY4R, or mouse NPY6R at concentrations of 10 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 328232-95-7
-
性状 Solid
-
分子量 406.41
-
分子式 C22H19FN4O3
-
Color Light yellow to light brown
-
SMILES
O=C([C@H]1CC[C@@](C2=C3C=CN=C2)(OC3=O)CC1)NC4=NN(C5=CC=CC=C5F)C=C4
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Ghrelin-induced neuronal NPY promotes brain metastasis in lung cancer patients with low BMI. [Abstract]2025 Jul 1;16(1):5608. PMID: 40595538
溶剤 & 溶解度
体外:
DMSO : 175 mg/mL (430.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
純度とドキュメンテーション
-
データシート (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Fichtner M, et al. Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2738-43. [Content Brief]
[2]. Erondu N, et al. Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults. Cell Metab. 2006 Oct;4(4):275-82. [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 | 2.4606 mL | 12.3028 mL | 24.6057 mL | 61.5142 mL |
| 5 mM | 0.4921 mL | 2.4606 mL | 4.9211 mL | 12.3028 mL | |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4606 mL | 6.1514 mL | |
| 15 mM | 0.1640 mL | 0.8202 mL | 1.6404 mL | 4.1009 mL | |
| 20 mM | 0.1230 mL | 0.6151 mL | 1.2303 mL | 3.0757 mL | |
| 25 mM | 0.0984 mL | 0.4921 mL | 0.9842 mL | 2.4606 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8202 mL | 2.0505 mL | |
| 40 mM | 0.0615 mL | 0.3076 mL | 0.6151 mL | 1.5379 mL | |
| 50 mM | 0.0492 mL | 0.2461 mL | 0.4921 mL | 1.2303 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4101 mL | 1.0252 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3076 mL | 0.7689 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2461 mL | 0.6151 mL |
MK-0557 関連分類
HY-15411 関連分類
Powered by Bioz