| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Luteinizing hormone receptor (LH-R), a G protein-coupled receptor (GPCR) found primarily on the surface of cells in the ovaries and testes. Luteinizing hormone (LH) binding to its receptor triggers a cascade of events leading to ovulation and testosterone production. As an antagonist, BAY-899 binds to the receptor and blocks its activation by LH, thereby inhibiting downstream signaling.
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| ln Vitro |
BAY-899 potently inhibits the activity of the luteinizing hormone receptor (LH-R). It exhibits IC50 values of 185 nM for the human LH receptor and 46 nM for the rat LH receptor. As a selective antagonist, it blocks the binding of LH to its receptor, preventing receptor activation and subsequent signaling. (R)-BAY-899 is the active enantiomer used in these assays.
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| ln Vivo |
In vivo activity data for BAY-899 is not detailed, but as an orally active antagonist of LH-R, it has potential applications in hormone-dependent diseases. By blocking LH-R, BAY-899 could potentially reduce the production of sex hormones. This makes it a candidate for treating conditions like uterine fibroids, endometriosis, prostate cancer, and precocious puberty.
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| Enzyme Assay |
A radioligand binding assay using membranes from cells expressing the LH receptor is performed. Membrane preparations are incubated with a radiolabeled ligand, such as [125I]-labeled hLH or a specific small molecule tracer, and various concentrations of the test compound. After incubation to reach equilibrium, the mixture is filtered to separate bound from free ligand, and the radioactivity on the filter is counted to determine the IC50.
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| Cell Assay |
A functional assay using cells that express the LH receptor and a reporter gene is used. These cells are treated with a sub-maximal concentration of LH to activate the receptor, leading to an increase in reporter signal (e.g., luciferase). The test compound is added to block this activation, and the decrease in signal is measured to determine its antagonistic potency (IC50).
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| Animal Protocol |
For in vivo efficacy studies, BAY-899 can be tested in a rat model of polycystic ovary syndrome (PCOS) or a mouse model of ovarian hyperstimulation syndrome (OHSS). For example, female rats treated with gonadotropins to induce ovarian folliculogenesis are administered BAY-899 orally. Endpoints include serum hormone levels (LH, progesterone), ovarian weight, and histological analysis of ovarian follicle development and luteinization.
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| ADME/Pharmacokinetics |
BAY-899 is an orally active compound with good solubility. It is freely soluble in DMSO at 125 mg/mL. For in vivo administration, it can be formulated in a vehicle such as DMSO, PEG300, Tween-80, and saline to achieve a clear solution for oral gavage or intraperitoneal injection. Detailed PK parameters such as half-life and bioavailability are not provided but are typical for an orally bioavailable small molecule antagonist.
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| Toxicity/Toxicokinetics |
Toxicity data for (R)-BAY-899 is not publicly available. As a research compound, it is intended for laboratory use only. The safety profile of LH-R antagonists is being studied for various clinical applications. Common side effects associated with this class of drugs include hot flashes, mood changes, and injection site reactions. No significant off-target toxicities have been reported in the literature.
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| References | |
| Additional Infomation |
BAY-899 is a research-grade chemical used to study the luteinizing hormone receptor. Its high selectivity for human and rat LH-R makes it a valuable tool for endocrine research. This product is for research use only and is not FDA-approved for human use. A key reference is likely a patent or paper from Bayer.
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| Molecular Formula |
C25H19F2N5O2
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|---|---|
| Molecular Weight |
459.45
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| CAS # |
2988191-40-6
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| Related CAS # |
BAY-899;2471967-92-5
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| Appearance |
Off-white to light yellow solid powder
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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 :~125 mg/mL (~272.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. 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 (10.88 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 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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 (10.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1765 mL | 10.8826 mL | 21.7652 mL | |
| 5 mM | 0.4353 mL | 2.1765 mL | 4.3530 mL | |
| 10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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