Linzagolix choline
Based on 1 Customer Validation
Linzagolix choline (KLH-2109 choline) is an orally active GnRH receptor antagonist with Ki values of 27.4 nM and 274.0 nM for the human and rat GnRH receptors, respectively. Linzagolix choline binds to GnRH1R, blocks GnRH signaling, and inhibits the hypothalamic-pituitary-gonadal axis. Linzagolix choline can be used in research on endometriosis, uterine fibroids, benign prostatic hyperplasia, and polycystic ovary syndrome.
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 : 99.60%
- CAS 番号: 1321816-57-2
- 分子式: C27H28F3N3O8S
- 分子量:611.59
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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
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
製品説明
IC50 & Target
[3]|
Human GnRH 27.4 nM (Ki) |
Rat GnRH 274 nM (Ki) |
体外実験
Linzagolix choline is a potent antagonist of the canine GnRH receptor in transfected 293 cells, with an IC50 of 79.5 nM[4].
Linzagolix choline exhibits potent concentration-dependent antagonism of human and cynomolgus monkey GnRH receptors at multiple concentrations in the HEK293 Ca2+ flux assay, with an IC50 value of 36.7 nM for the human GnRH receptor and an IC50 value of 441.9 nM for the monkey GnRH receptor[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Linzagolix (25-100 mg/kg; p.o.; single administration) choline inhibits serum estradiol concentrations in female rats after oral administration[3].
Linzagolix (10-100 mg/kg; p.o.; single dose) choline dose-dependently inhibits GnRH agonist-stimulated LH secretion in male rats, and the duration of inhibition is prolonged with increasing dose[4].
Linzagolix (1.25-5 mg/kg; p.o.; single dose) choline produces dose-dependent suppression of serum testosterone in healthy male dogs, with the 5 mg/kg dose maintaining testosterone below the lower limit of quantification within 24 h[4].
Linzagolix (5 mg/kg; p.o.; once daily; 28 days) choline maintains testosterone suppression and significantly reduces prostate weight in dogs with benign prostatic hyperplasia[4].
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, 10 weeks old at model preparation; Charles River Japan)[3]
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Dosage:50 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:p.o.; twice daily; 14 days
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Result:Cyst volumes were decreased compared with the control group at 50, 100, and 200 mg/kg.
The lowest dose showing decreased cyst volume was 50 mg/kg.
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Animal Model:Sprague-Dawley (female, 11 weeks old)[3]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; single administration
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Result:Serum E2 concentrations were suppressed dose-dependently at 25, 50, and 100 mg/kg compared with vehicle up to 24 h after oral administration.
At 24 h, E2 concentrations in the 25 mg/kg group had recovered to 80% of the vehicle group.
A recovery trend was observed at 50 mg/kg at 24 h.
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Animal Model:Sprague-Dawley (male)[4]
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Dosage:10, 30 and 100 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited leuprolide-induced LH secretion in a dose-dependent manner; the significant effect persisted up to 12 h after administration in the 10 mg/kg group and up to 16 h after administration in the 30 and 100 mg/kg groups compared with the vehicle control group.
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Animal Model:Beagle (male; 12 months old)[4]
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Dosage:1.25, 2.5 and 5 mg/kg
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Administration:p.o.; single dose
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Result:Serum testosterone levels showed a circadian rhythm in the vehicle control group, with the lowest levels at approximately noon.
Suppressed serum testosterone concentrations in a dose-dependent manner; serum testosterone levels were below the limit of quantitation up to 12 h after administration of 1.25 and 2.5 mg/kg and up to 24 h after 5 mg/kg.
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Animal Model:Beagle (male; 44-90 months old at start of administration)[4]
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Dosage:5 mg/kg
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Administration:p.o.; once daily; 28 days
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Result:Serum testosterone levels were constantly reduced throughout the 28-day dosing period (measured on days 1 and 28).
After 4 weeks of repeated administration, prostate weight per body weight was decreased by 41% compared with the control group.
Testis weight showed a downward trend (decreased by 24%) compared with the control group.
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Animal Model:Sprague-Dawley (female; 10 weeks old at PCOS model preparation)[4]
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Dosage:200 mg/kg (200×2 mg/kg/day)
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Administration:p.o.; twice daily; 14 days
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Result:In Letrozole-exposed control rats, polycystic formation was significantly increased and corpora lutea decreased.
Significantly decreased the number of follicular cysts (9.8 vs control 20.7; normal 1.1) and increased the number of corpora lutea (33.9 vs control 25.3; normal 40.6).
In the insulin tolerance test, the change in blood glucose levels (0-1 h) was 39.8 mg/dL versus 26.4 mg/dL in the control group, indicating significantly reduced insulin resistance.
Serum FSH was significantly decreased (8.96 ng/mL vs control 11.74; normal 6.65), whereas LH (1.40 vs control 2.35; normal 1.03 ng/mL), LH/FSH ratio (0.15 vs control 0.21; normal 0.16) and testosterone (210.99 vs control 146.12; normal 4.00 ng/dL) were not significantly decreased.
化学情報
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CAS 番号 1321816-57-2
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性状 Solid
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分子量 611.59
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分子式 C27H28F3N3O8S
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Color White to off-white
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SMILES
OCC[N+](C)(C)C.O=C([O-])C1=C(C(NC2=O)=CS1)C(N2C3=CC(OCC4=C(C=CC(F)=C4F)OC)=C(C=C3F)OC)=O
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別名
KLH-2109 choline; OBE-2109 choline
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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
体外:
DMSO : 5.83 mg/mL (9.53 mM; ultrasonic and warming and heat to 60°C; 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)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (297 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)
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- 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
[2]. Kobayashi K, et al. Non-clinical studies indicating lack of interactions between iron/calcium ions and linzagolix, an orally available GnRH antagonist. Xenobiotica. 2022 May;52(5):488-497. [Content Brief]
[3]. Tezuka M, et al. Suppressive effects of linzagolix, a novel non-peptide antagonist of gonadotropin-releasing hormone receptors, in experimental endometriosis model rats. Clinical and experimental pharmacology & physiology. 2023 Jul;50(7):610-617. [Content Brief]
[4]. Tezuka M, et al. Suppression of hypothalamic-pituitary-gonadal function by linzagolix in benign prostatic hyperplasia and polycystic ovary syndrome animal models. Clinical and experimental pharmacology & physiology. 2023 Nov;50(11):914-923. [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 | 1.6351 mL | 8.1754 mL | 16.3508 mL | 40.8771 mL |
| 5 mM | 0.3270 mL | 1.6351 mL | 3.2702 mL | 8.1754 mL |
Linzagolix choline 関連分類
HY-120767 関連分類
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Keywords
- Linzagolix
- 1321816-57-2
- KLH-2109
- OBE-2109
- KLH2109
- KLH 2109
- OBE2109
- OBE 2109
- GnRH Receptor
- Gonadotropin releasing hormone receptor
- GNRHR
- GnRH receptor antagonist
- endometriosis
- follicle-stimulating hormone
- gonadotropin secretion
- hypothalamic-pituitary-gonadal axis
- luteinizing hormone
- oestradiol
- polycystic ovary syndrome
- testosterone
- uterine fibroids
- Inhibitor
- inhibitor
- inhibit