Acyline
Based on 1 Customer Validation
Acyline, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels.
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: 99.52%
- CAS 番号: 170157-13-8
- 分子式: C80H102ClN15O14
- 分子量:1533.21
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.52 nM
Compound: 8
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Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
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[PMID: 17402723] |
| HEK293 | IC50 |
0.69 nM
Compound: 2
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Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
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[PMID: 16759096] |
| HEK293 | IC50 |
1.5 nM
Compound: 8
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Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
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[PMID: 17402723] |
| HEK293 | IC50 |
6.8 nM
Compound: 6 (Acyline)
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Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
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[PMID: 11462984] |
| Mast cell | EC50 |
461.4 μg/mL
Compound: 2
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Histamine release in mast cells by ELISA
Histamine release in mast cells by ELISA
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[PMID: 16759096] |
Acyline (50 μg, s.c., once) can reduce FSH concentrations from pre-acyline 1.51 ng/mL to post-acyline 1.27 ng/mL in male Kiss1−/− mice and from pre-acyline 2.87 ng/mL to post-acyline 1.95 ng/mL in male Gpr54−/− mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Kiss1−/−and Gpr54−/− mice[1]
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Dosage:50 μg (1 mg/mL in PBS)
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Administration:Subcutaneous injection; twice daily; 5 days
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Result:12 Kiss1−/− mice left oestrus within 4 days of 13 mice received acyline while only 2 of 17 mice received vehicle left oestrus. Also, 7 of 8 Gpr54−/− mice received acyline left oestrus compared to 1 of 7 received vehicle.
Reduced uterine weights of Kiss1−/−and Gpr54−/− mice in treated group compared to the vehicle group, and reduced serum LH concentrations in Kiss1−/− mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 170157-13-8
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性状 Solid
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分子量 1533.21
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分子式 C80H102ClN15O14
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Color White to off-white
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
H2O : 3.33 mg/mL (2.17 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (274 KB)
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SDS (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.6522 mL | 3.2611 mL | 6.5223 mL | 16.3057 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Acyline 関連分類
HY-16027 関連分類
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