Linzagolix
Based on 1 Customer Validation
Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 935283-04-8
- Formula: C22H15F3N2O7S
- Molecular Weight:508.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Lindagolix reduces serum luteinizing hormone and testosterone levels in male rats and dogs with normal or BPH models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Endometriosis model rat[1]
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Dosage:50 mg/kg
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Administration:
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Result:Reduced cyst volume.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 935283-04-8
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Appearance Solid
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Molecular Weight 508.42
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Formula C22H15F3N2O7S
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Color White to light brown
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SMILES
O=C(C(SC=C1NC(N2C3=C(F)C=C(OC)C(OCC4=C(C(F)=CC=C4OC)F)=C3)=O)=C1C2=O)O
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Synonyms
KLH-2109; OBE-2109
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (245.86 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Motohiro Tezuka, et al. Suppressive effects of linzagolix, a novel non-peptide antagonist of gonadotropin-releasing hormone receptors, in experimental endometriosis model rats. Clin Exp Pharmacol Physiol. 2023 Jul;50(7):610-617. [Content Brief]
[2]. Motohiro Tezuka, et al. Suppression of hypothalamic-pituitary-gonadal function by linzagolix in benign prostatic hyperplasia and polycystic ovary syndrome animal models. Clin Exp Pharmacol Physiol. 2023 Nov;50(11):914-923. [Content Brief]
[3]. Susan Dababou, et al. Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas. Expert Opin Investig Drugs. 2021 Sep;30(9):903-911. [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 | 1.9669 mL | 9.8344 mL | 19.6688 mL | 49.1719 mL |
| 5 mM | 0.3934 mL | 1.9669 mL | 3.9338 mL | 9.8344 mL | |
| 10 mM | 0.1967 mL | 0.9834 mL | 1.9669 mL | 4.9172 mL | |
| 15 mM | 0.1311 mL | 0.6556 mL | 1.3113 mL | 3.2781 mL | |
| 20 mM | 0.0983 mL | 0.4917 mL | 0.9834 mL | 2.4586 mL | |
| 25 mM | 0.0787 mL | 0.3934 mL | 0.7868 mL | 1.9669 mL | |
| 30 mM | 0.0656 mL | 0.3278 mL | 0.6556 mL | 1.6391 mL | |
| 40 mM | 0.0492 mL | 0.2459 mL | 0.4917 mL | 1.2293 mL | |
| 50 mM | 0.0393 mL | 0.1967 mL | 0.3934 mL | 0.9834 mL | |
| 60 mM | 0.0328 mL | 0.1639 mL | 0.3278 mL | 0.8195 mL | |
| 80 mM | 0.0246 mL | 0.1229 mL | 0.2459 mL | 0.6146 mL | |
| 100 mM | 0.0197 mL | 0.0983 mL | 0.1967 mL | 0.4917 mL |