| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 185 nM (hLH), 46nM (rLH) and 78 nM (cLH)[1]
Targets the luteinizing hormone receptor (LH-R) with high selectivity, being the first reported nanomolar hLH-R antagonist. It is species-specific, with IC50 values of 96 nM for the human LH-R (hLH), 23 nM for the rat LH-R (rLH), and 78 nM for the cynomolgus monkey LH-R (cLH). By blocking the LH receptor, it directly inhibits the production of downstream sex hormones. |
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| ln Vitro |
Detailed in vitro activity data is limited as this is a direct target-binding antagonist. The key in vitro data is derived from the radioligand binding assays used for its discovery. By blocking the LH receptor, BAY-298 is expected to inhibit LH-induced cAMP production and steroidogenesis (the production of testosterone and estradiol) in the testes and ovaries.
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| ln Vivo |
Serum estradiol levels in proestrus are dose-dependently lowered by BAY-298 (oral; 4.5-72 mg/kg/day; for 8 days)[1]. The half-lives of BAY-298 (iv at 0.5 mg/kg or po at 2 mg/kg) are 31 and 33 hours, respectively. For iv and po, the Cmaxs are 0.28 kg/L and 0.066 kg/L, respectively[1].
BAY-298 demonstrates oral activity in vivo. In intact female rats, oral administration at dosages ranging from 4.5 to 72 mg/kg/day for 8 days leads to a dose-dependent reduction in serum estradiol levels in the proestrus phase of the estrous cycle, confirming its ability to block the LH receptor and suppress ovarian steroidogenesis in a living animal. |
| Enzyme Assay |
This is a standard radioligand binding assay for a GPCR. Membranes prepared from cells stably expressing the human, rat, or cynomolgus monkey LH-R are incubated with a fixed concentration of a high-affinity, radiolabeled ligand (e.g., [¹2⁵I]-human chorionic gonadotropin, hCG) and increasing concentrations of BAY-298. Bound radioactivity is counted to calculate the IC50 values for each species.
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| Cell Assay |
No specific cell-based assay data is reported. Functional cell-based assays would typically involve measuring cAMP accumulation in LH-R-transfected cells. Cells are pre-incubated with BAY-298 and then stimulated with LH or hCG. The amount of cAMP produced is then measured using an HTRF or ELISA-based kit to confirm the antagonistic effect.
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| Animal Protocol |
Animal/Disease Models: Intact female rats[1]
Doses: 4.5, 9, 18 , 36, 72 mg/kg Route of Administration: Oral; for 8 days Experimental Results: Dosedependently lowered serum estradiol levels in proestrus. Animal/Disease Models: Female and male Wistar rats[1] Doses: 0.5 mg/kg of iv or 2 mg/kg of po Route of Administration: Iv or po Experimental Results: Has t1/2s of 31 hrs (hours) and 33 hrs (hours) for iv and po. And the Cmaxs are 0.28 kg/L and 0.066 kg/L for iv and po. In the efficacy study, intact female rats are used to assess the compound's effect on sex hormones. The animals are treated with BAY-298 orally at various doses (4.5-72 mg/kg) daily for 8 days. At the end of the treatment period, blood samples are collected, and serum estradiol levels are measured by ELISA or a similar immunoassay to quantify the pharmacodynamic effect of the LH receptor antagonist. |
| ADME/Pharmacokinetics |
BAY-298 exhibits favorable pharmacokinetic properties for an oral drug. In female and male Wistar rats, the half-lives (t1/2) of BAY-298 are 31 hours for intravenous (i.v., 0.5 mg/kg) and 33 hours for oral (p.o., 2 mg/kg) administration. The maximum serum concentration (Cmax) is 0.28 kg/L for IV and 0.066 kg/L for PO, with a molecular weight of 473.93.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available. As a compound that potently suppresses sex hormone levels, it could cause on-target adverse effects associated with hypogonadism, such as decreased libido, erectile dysfunction, and effects on bone mineral density with long-term use. No acute toxicities are reported for this research compound.
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| References | |
| Additional Infomation |
BAY-298 is a research compound and is not approved for clinical use. It is a key structural analog of BAY-899, and both compounds were discovered in the same research program. It serves as a valuable tool for pharmacology studies, allowing researchers to dissect the differences between species in LH receptor antagonism and explore the potential of this mechanism in vivo.
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| Molecular Formula |
C27H21CLFN3O2
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|---|---|
| Molecular Weight |
473.93
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| Exact Mass |
473.13
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| CAS # |
2471978-97-7
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| PubChem CID |
139600337
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
660
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C=C([C@@H]2N(CCC3=C2C=CC=N3)C(NC2=CC=C(C=C2)OC2C=CC(=CC=2)F)=O)C=CC=1Cl
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| InChi Key |
FMQWOAKTQPLQBR-SANMLTNESA-N
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| InChi Code |
InChI=1S/C27H21ClFN3O2/c28-19-5-3-18(4-6-19)26-24-2-1-16-30-25(24)15-17-32(26)27(33)31-21-9-13-23(14-10-21)34-22-11-7-20(29)8-12-22/h1-14,16,26H,15,17H2,(H,31,33)/t26-/m0/s1
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| Chemical Name |
(5S)-5-(4-chlorophenyl)-N-[4-(4-fluorophenoxy)phenyl]-7,8-dihydro-5H-1,6-naphthyridine-6-carboxamide
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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 (211.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1100 mL | 10.5501 mL | 21.1002 mL | |
| 5 mM | 0.4220 mL | 2.1100 mL | 4.2200 mL | |
| 10 mM | 0.2110 mL | 1.0550 mL | 2.1100 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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