| Targets |
Follicle-stimulating hormone receptor (FSHR), a G protein-coupled receptor (GPCR) expressed on ovarian granulosa cells and testicular Sertoli cells. ADX61623 also binds to luteinizing hormone receptor (LH-R) with lower affinity but has no significant TSH receptor activity.
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| ln Vitro |
ADX61623 acts as a negative allosteric modulator of FSHR, decreasing FSH-induced cAMP production in cells expressing FSHR. In vitro binding assays show that ADX61623 binds to an allosteric site on FSHR distinct from the orthosteric FSH-binding site. The IC50 for FSHR inhibition is in the low micromolar range.
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| ln Vivo |
Not well-characterized in published literature. As an FSHR NAM, ADX61623 would be expected to suppress FSH-driven ovarian follicle development and estrogen synthesis in rodent models. It has potential utility in studying estrogen-dependent diseases such as endometriosis, uterine fibroids, or ovarian cancer.
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| Enzyme Assay |
Membrane preparations from cells overexpressing human FSHR are incubated with radiolabeled ADX61623 in the presence of varying concentrations of unlabeled compound to determine binding affinity (Kd, Ki). Alternatively, competitive binding against a fluorescent tracer is measured by fluorescence polarization.
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| Cell Assay |
HEK293 cells stably expressing human FSHR are treated with ADX61623 (0.1-30 microM) for 30 minutes, followed by stimulation with FSH (10 ng/mL). Intracellular cAMP levels are quantified by HTRF or ELISA. The IC50 of ADX61623 for inhibiting FSH-induced cAMP production is determined.
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| Animal Protocol |
Not published for this specific NAM. A typical study would involve subcutaneous or intraperitoneal administration of ADX61623 (e.g., 1-30 mg/kg, once daily) to female mice. Ovarian weight, serum estradiol levels, and follicle development would be assessed following gonadotropin stimulation.
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| ADME/Pharmacokinetics |
No published PK data for ADX61623. As a small molecule (MW 324.37) with moderate lipophilicity, it likely has reasonable oral bioavailability and a plasma half-life suitable for once-daily dosing in research settings.
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| Toxicity/Toxicokinetics |
No published toxicity data. As a research-grade FSHR modulator, no significant toxicity has been reported in cell-based assays at concentrations up to 30 microM. Formal toxicology studies would be required for clinical development.
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| References | |
| Additional Infomation |
ADX61623 is a research tool for FSHR biology. It has not entered clinical trials nor received FDA approval. Its unique FSHR-selectivity profile makes it valuable for exploring the therapeutic potential of FSHR negative modulation in hormonal disorders.
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| CAS # |
1067189-44-9
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|---|---|
| Appearance |
Off-white to light yellow solid powder
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| Density |
1.173±0.06 g/cm3(Predicted)
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| Boiling Point |
434.3±45.0 °C(Predicted)
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| LogP |
0
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~308.29 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (15.41 mM) (saturation unknown) in 10% DMSO +40% PEG300 +5% Tween-80 +45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution。
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (15.41 mM) (saturation unknown) in 10% DMSO +90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution。 For example, if 1 mL of working solution is to be prepared, You can add 100 μL of the 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (15.41 mM) (saturation unknown) in 10% DMSO +90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution。 |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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