GTX-758
Based on 1 Customer Validation
GTX-758 (Capesaris) is an orally active and selective ERα activator with an EC50 of 2.1 nM. GTX-758 activates ERα- and ERβ-mediated transcription, inhibits the hypothalamic-pituitary-gonadal axis to reduce serum LH, FSH, and testosterone levels, and reversibly reduces serum testosterone to castration levels. GTX-758 exerts anti-resorptive effects on trabecular bone, alleviates hot flash-like vasomotor responses, reduces prostate volume, and lowers circulating prostate-specific antigen levels. GTX-758 reduces fat mass and body weight and increases trabecular bone volume in aged intact male rats. GTX-758 can be used in research related to prostate cancer.
For research use only. We do not sell to patients.
- Purity : 99.59%
- CAS No.: 938067-78-8
- Formula: C19H13F2NO3
- Molecular Weight:341.31
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ERα 2.1 nM (EC50) |
ERβ 27 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
2.1 nM
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ERα transcriptional activation in COS-7 cells assessed by luciferase reporter assay with exposure 24 hrs after transfection and measurement 48 hrs after exposure.
ERα transcriptional activation in COS-7 cells assessed by luciferase reporter assay with exposure 24 hrs after transfection and measurement 48 hrs after exposure.
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22294742 |
| COS-7 | EC50 |
27 nM
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ERβ transcriptional activation in COS-7 cells assessed by luciferase reporter assay with exposure 24 hrs after transfection and measurement 48 hrs after exposure.
ERβ transcriptional activation in COS-7 cells assessed by luciferase reporter assay with exposure 24 hrs after transfection and measurement 48 hrs after exposure.
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22294742 |
| Ishikawa | EC50 |
1.15 nM
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Alkaline phosphatase induction in Ishikawa endometrial adenocarcinoma cells as a measure of endometrial cell growth and differentiation.
Alkaline phosphatase induction in Ishikawa endometrial adenocarcinoma cells as a measure of endometrial cell growth and differentiation.
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22294742 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GTX-758 (0.3-30 mg/kg/d; s.c.; daily; 14 d) inhibits LH and FSH in castrated male rats[1].
GTX-758 (1-30 mg/kg; p.o.; daily; 3 d) reduces serum testosterone in intact male rats[1].
GTX-758 (10 mg/kg; s.c.; single administration) rapidly suppresses LH in castrated rats[1].
GTX-758 (10-30 mg/kg/d; 7 d) attenuates ovariectomy-induced withdrawal-evoked elevation of tail skin temperature in rats[1].
GTX-758 (1-30 mg/kg/d; 42 d) reduces androgen-dependent tissue weight and increases trabecular bone volume at castration doses in aged rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat (male, 7 weeks, 200 g)[1]
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Dosage:0.3, 1, 3, 10, and 30 mg/kg/d
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Administration:s.c.; daily; 14 d
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Result:Reduced serum testosterone and androgen-dependent tissue weights in intact male rats.
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Animal Model:Rat (male, 7 weeks, 200 g, were surgically castrated and allowed to recover)[1]
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Dosage:0.3, 1, 3, 10, and 30 mg/kg/d
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Administration:s.c.; daily; 14 d
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Result:Suppressed LH and FSH in orchidectomized male rats.
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Animal Model:Rat (male, 7 weeks, 200 g)[1]
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Dosage:1, 3, and 30 mg/kg
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Administration:p.o. (oral gavage); daily; 3 d
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Result:Reduced serum testosterone in intact male rats.
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Animal Model:Cynomolgus monkeys (Sexually mature, male, 5-6 yr of age and weighed between 5.8 and 8.1 kg)
[1] -
Dosage:1, 10, and 100 mg/kg
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Administration:p.o.; once daily; up to 39 wk
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Result:Produced reversible castration-level testosterone suppression and reduces prostate volume, PSA, and bone turnover markers in male Cynomolgus monkeys without increased platelet reactivity.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 938067-78-8
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Appearance Solid
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Molecular Weight 341.31
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Formula C19H13F2NO3
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Color White to off-white
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SMILES
O=C(N(C1=CC=C(F)C=C1)C2=CC=C(O)C=C2)C3=CC=C(O)C(F)=C3
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Synonyms
Capesaris
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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
In Vitro:
DMSO : 100 mg/mL (292.99 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)
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
Purity & Documentation
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Data Sheet (289 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.9299 mL | 14.6494 mL | 29.2989 mL | 73.2472 mL |
| 5 mM | 0.5860 mL | 2.9299 mL | 5.8598 mL | 14.6494 mL | |
| 10 mM | 0.2930 mL | 1.4649 mL | 2.9299 mL | 7.3247 mL | |
| 15 mM | 0.1953 mL | 0.9766 mL | 1.9533 mL | 4.8831 mL | |
| 20 mM | 0.1465 mL | 0.7325 mL | 1.4649 mL | 3.6624 mL | |
| 25 mM | 0.1172 mL | 0.5860 mL | 1.1720 mL | 2.9299 mL | |
| 30 mM | 0.0977 mL | 0.4883 mL | 0.9766 mL | 2.4416 mL | |
| 40 mM | 0.0732 mL | 0.3662 mL | 0.7325 mL | 1.8312 mL | |
| 50 mM | 0.0586 mL | 0.2930 mL | 0.5860 mL | 1.4649 mL | |
| 60 mM | 0.0488 mL | 0.2442 mL | 0.4883 mL | 1.2208 mL | |
| 80 mM | 0.0366 mL | 0.1831 mL | 0.3662 mL | 0.9156 mL | |
| 100 mM | 0.0293 mL | 0.1465 mL | 0.2930 mL | 0.7325 mL |
GTX-758 Related Classifications
HY-111061 Related Classifications
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