PF-04628935
Based on 1 Customer Validation
PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research.
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: 99.58%
- CAS 番号: 1383719-97-8
- 分子式: C24H26ClN7OS
- 分子量:496.03
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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GHSR1a 4.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4.6 nM
Compound: 10n
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Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
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[PMID: 22677316] |
化学情報
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CAS 番号 1383719-97-8
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性状 Solid
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分子量 496.03
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分子式 C24H26ClN7OS
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Color Light yellow to yellow
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SMILES
CC1=CN2C(S1)=NC(CC(N3CCC4(CN(C4)CC5=CC=C(C=C5Cl)N6N=CC=N6)CC3)=O)=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (100.80 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 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)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kung DW, et, al. Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. [Content Brief]
[2]. Cavalcante DP, et, al. Role of dorsal raphe nucleus GHS-R1a receptors in the regulation of inhibitory avoidance and escape behaviors in rats. Behav Brain Res. 2019 Jun 3;365:178-184. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0160 mL | 10.0800 mL | 20.1601 mL | 50.4002 mL |
| 5 mM | 0.4032 mL | 2.0160 mL | 4.0320 mL | 10.0800 mL | |
| 10 mM | 0.2016 mL | 1.0080 mL | 2.0160 mL | 5.0400 mL | |
| 15 mM | 0.1344 mL | 0.6720 mL | 1.3440 mL | 3.3600 mL | |
| 20 mM | 0.1008 mL | 0.5040 mL | 1.0080 mL | 2.5200 mL | |
| 25 mM | 0.0806 mL | 0.4032 mL | 0.8064 mL | 2.0160 mL | |
| 30 mM | 0.0672 mL | 0.3360 mL | 0.6720 mL | 1.6800 mL | |
| 40 mM | 0.0504 mL | 0.2520 mL | 0.5040 mL | 1.2600 mL | |
| 50 mM | 0.0403 mL | 0.2016 mL | 0.4032 mL | 1.0080 mL | |
| 60 mM | 0.0336 mL | 0.1680 mL | 0.3360 mL | 0.8400 mL | |
| 80 mM | 0.0252 mL | 0.1260 mL | 0.2520 mL | 0.6300 mL | |
| 100 mM | 0.0202 mL | 0.1008 mL | 0.2016 mL | 0.5040 mL |