| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
IC50: 185 nM (hLH), 46nM (rLH) and 78 nM (cLH)[1]
|
|---|---|
| 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].
|
| 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. |
| References |
[1]. Wortmann L, et al. Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels In Vivo. J Med Chem. 2019 Oct 31.
|
| Molecular Formula |
C27H21CLFN3O2
|
|---|---|
| Molecular Weight |
473.93
|
| CAS # |
2471978-97-7
|
| 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
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (211.00 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
