ADX68692
ADX68692 is an orally active FSHR negative allosteric regulator, with an IC50 value of 140 nM against hFSHR. ADX68692 antagonizes hCG (HY-107953)-mediated cAMP production, β-arrestin 2 recruitment, and the LH/CGR signaling pathway. ADX68692 partially inhibits testosterone synthesis. ADX68692 blocks follicle growth, disrupts the estrous cycle in rats, and reduces the pregnancy rate in rats. ADX68692 can be used in research related to contraception and endometriosis.
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- No. CAS: 1067191-08-5
- Fòrmula: C24H23N3O3
- Peso molecular:401.46
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
ADX68692 acts as a negative allosteric modulator of LHCGR, inhibiting hCG-mediated cAMP production and β-arrestin 2 recruitment in HEK293 cells, mLTC-1 cells, and rat primary Leydig cells, while exerting cell-specific effects on steroid production that include increased progesterone and partially inhibited testosterone synthesis in rat primary Leydig cells[1].
ADX68692 (20 min) dose-dependently inhibits FSH-induced cAMP production in HEK293 cells stably expressing FSHR with a pIC50 of 5.71[2].
ADX68692 (10 μM; 1 h) reduces the maximal hCG-induced CRE-driven luciferase response to 55.89% of control in HEK293 cells transiently expressing LH/CGR and pSOM-Luc[2].
ADX68692 (10 μM; 1 h) does not inhibit hCG-induced progesterone production in mLTC-1 cells endogenously expressing LH/CGR[2].
ADX68692 is a negative allosteric modulator of FSHR, with highest potency at hFSHR (IC50 = 140 nM), moderate potency at rFSHR (IC50 = 207 nM), weak activity at hLHR (IC50 = 804 nM), and no activity at hTSHR[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ADX68692 (10-100 mg/kg; s.c., p.o.; twice daily; 2 days) dose-dependently inhibits FSH-induced oocyte ovulation in immature female rats when administered subcutaneously or orally, with an ~85% reduction in ovulated oocytes at subcutaneous doses of 50 and 100 mg/kg, and significant inhibition at all tested oral doses, without altering ovarian weight gain[3].
ADX68692 (10-25 mg/kg; p.o.; twice daily) disrupts estrous cycles in mature female rats at oral doses of 10 and 25 mg/kg, and reduces the percentage of mated rats that conceive, without affecting the number of implantation sites in rats that do conceive[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar Hanover or Sprague-Dawley (immature female, 22 days of age, induced ovulation via exogenous hFSH followed by hCG)[3]
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Dosage:100 mg/kg; 50 mg/kg; 30 mg/kg; 50 mg/kg; 25 mg/kg; 10 mg/kg
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Administration:s.c.; twice daily; 2 days; p.o.; twice daily; 2 days
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Result:Caused an ~85% decrease in the average number of oocytes recovered per ampulla (from ~9 to 1.4 oocytes) relative to controls (P < 0.001) at subcutaneous doses of 50 mg/kg and 100 mg/kg.
Failed to produce a statistically significant reduction in oocyte recovery at subcutaneous dose of 30 mg/kg.
Significantly reduced oocyte recovery relative to controls (P < 0.05) at all tested oral doses: controls yielded 16.0 oocytes per ampulla, while 50 mg/kg-treated rats yielded 2.10 oocytes per ampulla, and 25 mg/kg-treated rats yielded 0.1 oocytes per ampulla.
Had no significant effect on FSH-induced ovarian weight gain at any tested dose via either route.
Chemical Information
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No. CAS 1067191-08-5
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Peso molecular 401.46
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Fòrmula C24H23N3O3
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SMILES
CC(C(C(C1=CN=CC=C1)=C2)=CC=C2NC(C3=CC=C(OC)C(OC)=C3)=O)(C#N)C
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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]. Lazzaretti C, et al. Allosteric modulation of gonadotropin receptors. Frontiers in endocrinology. 2023;14:1179079. [Content Brief]
[2]. Ayoub MA, et al. Profiling of FSHR negative allosteric modulators on LH/CGR reveals biased antagonism with implications in steroidogenesis. Molecular and cellular endocrinology. 2016 Nov 15;436:10-22. [Content Brief]
[3]. Dias JA, et al. Inhibition of follicle-stimulating hormone-induced preovulatory follicles in rats treated with a nonsteroidal negative allosteric modulator of follicle-stimulating hormone receptor. Biol Reprod. 2014 Jan 30;90(1):19. . [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ADX68692 Related Classifications
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