Teverelix
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
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- No. CAS: 151272-78-5
- Fòrmula: C74H100ClN15O14
- Peso molecular:1459.13
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Teverelix (10 nM, 45 mins) inhibits GnRH-induced intracellular Ca2+ increase in HEK293/GnRHR cells[2].
Teverelix (0.1 nM-1 μM, 45 mins) inhibits GnRH-induced cAMP accumulation in HEK293/GnRHR cells[2].
Teverelix (10 nM-1 μM, 15 mins) inhibits GnRH-induced pERK1/2 and pCREB activation in HEK293/GnRHR cells[2].
Teverelix inhibits histamine release in a peritoneal rat mast cell, with an EC50value of 81 μg/mL[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293/GnRHR cells
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Concentration:10 nM, 100 nM, 1 μM
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Incubation Time:15 mins
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Result:Inhibited GnRH-induced pERK1/2 and pCREB activation.
Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[3]
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Dosage:300, 100, 30, 10 and 3 μg/kg
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Administration:Intramuscular injection
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Result:Showed dose-response and time-course of testosterone inhibitory activity.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 151272-78-5
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Peso molecular 1459.13
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Fòrmula C74H100ClN15O14
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Synonyms
EP 24332
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. MacLean CM, et al. Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix Trifluoroacetate, a Novel Gonadotropin-Releasing Hormone Antagonist, in Healthy Adult Subjects. Clin Pharmacol Drug Dev. 2022 Feb;11(2):257-269. [Content Brief]
[2]. Sperduti S, et al. GnRH Antagonists Produce Differential Modulation of the Signaling Pathways Mediated by GnRH Receptors. Int J Mol Sci. 2019 Nov 7;20(22):5548. [Content Brief]
[3]. Deghenghi R, et al. Antarelix (EP 24332) a novel water soluble LHRH antagonist. Biomed Pharmacother. 1993;47(2-3):107-10. [Content Brief]
[4]. Fraser HM, et al. Initiation of high dose gonadotrophin-releasing hormone antagonist treatment during the late follicular phase in the macaque abolishes luteal function irrespective of effects upon the luteinizing hormone surge. Hum Reprod. 1997 Mar;12(3):430-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Teverelix Related Classifications
HY-105173 Related Classifications
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