Ganirelix acetate
Based on 1 Customer Validation
Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity.
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: 99.19%
- CAS 番号: 129311-55-3
- 分子式: C84H121ClN18O17
- 分子量:1690.42
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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
GnRH[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
3.6 nM
Compound: 3 (Ganirelix)
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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] |
Ganirelix (1 nM-1 μM) acetate has no effect on Carbachol-induced or nerve-induced detrusor contractions in isolated bladder preparations from female rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ganirelix (1.4 mg/L; intravesical administration; single dose) acetate regulates normal micturition function in female rats by prolonging micturition intervals, increasing voided volume and bladder capacity, while reducing basal urodynamic pressure, threshold urodynamic pressure and maximum urodynamic pressure parameters; its reduction in flow pressure does not reach statistical significance[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female, 225-300 g, intravesical infusion of 50 μM prostaglandin E2-induced detrusor overactivity)[2]
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Dosage:0.1 mg/kg
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Administration:s.c.; daily; 14 days
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Result:Reduced plasma luteinising hormone (LH) levels to 0.48 ng/mL.
Reduced micturition interval (MI) by 22%.
Reduced micturition volume (MV) by 23%.
Reduced bladder capacity (BC) by 21% (.
Increased threshold pressure (TP) by 16%.
Increased flow pressure (FP) by 16%.
Enhanced maximal carbachol-induced contraction force to 231% of 60 mM K+-induced contractions at 10 μM Carbachol.
Showed no significant differences in body weight, bladder weight, or baseline urodynamic parameters compared to controls.
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Animal Model:Sprague-Dawley (female, 225-300 g)[2]
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Dosage:1.4 mg/L; 0.14 mg/L
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Administration:intravesical; single dose
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Result:Increased micturition interval (MI) to 7.06 min at 1.4 mg/L.
Increased micturition volume (MV) to 1.17 mL at 1.4 mg/L.
Increased bladder capacity (BC) to 1.17 mL 1.4 mg/L.
Reduced basal pressure (BP) to 21.5 cm H2O at 1.4 mg/L.
Reduced threshold pressure (TP) to 34.9 cm H2O at 1.4 mg/L.
Reduced maximum pressure (MP) to 126.0 cm H2O at 1.4 mg/L.
Reduced flow pressure (FP) with no statistical significance at 1.4 mg/L.
Showed no effect on any measured urodynamic parameters at 0.14 mg/L.
化学情報
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CAS 番号 129311-55-3
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性状 Solid
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分子量 1690.42
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分子式 C84H121ClN18O17
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Color White to off-white
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SMILES
OC(C=C1)=CC=C1C[C@H](NC([C@H](CO)NC([C@@H](CC2=CN=CC=C2)NC([C@H](NC([C@H](NC(C)=O)CC3=CC4=CC=CC=C4C=C3)=O)CC5=CC=C(Cl)C=C5)=O)=O)=O)C(N[C@H](CCCC/N=C(NCC)/NCC)C(N[C@@H](CC(C)C)C(N[C@@H](CCCC/N=C(NCC)/NCC)C(N6[C@@H](CCC6)C(N[C@H](C)C(N)=O)=O)=O)=O)=O)=O.CC(O)=O.CC(O)=O
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別名
Ganirest
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
H2O : 50 mg/mL (29.58 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (29.58 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (278 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[1]. Gustofson RL, et al. Ganirelix acetate causes a rapid reduction in estradiol levels without adversely affecting oocyte maturation in women pretreated with leuprolide acetate who are at risk of ovarian hyperstimulation syndrome. Hum Reprod. 2006;21(11):2830-2837. [Content Brief]
[2].
Russo A. et al. Effects of the gonadotropin-releasing hormone antagonist ganirelix on normal micturtion and prostaglandin
E(2)-induced detrusor overactivity in conscious female rats. Eur Urol. 2011;59(5):868-874.
[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 (protect from light, stored under nitrogen). 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 | 0.5916 mL | 2.9578 mL | 5.9157 mL | 14.7892 mL |
| 5 mM | 0.1183 mL | 0.5916 mL | 1.1831 mL | 2.9578 mL | |
| 10 mM | 0.0592 mL | 0.2958 mL | 0.5916 mL | 1.4789 mL | |
| 15 mM | 0.0394 mL | 0.1972 mL | 0.3944 mL | 0.9859 mL | |
| 20 mM | 0.0296 mL | 0.1479 mL | 0.2958 mL | 0.7395 mL | |
| 25 mM | 0.0237 mL | 0.1183 mL | 0.2366 mL | 0.5916 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.
Ganirelix acetate 関連分類
HY-109532 関連分類
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