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  3. BAY-298

BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels.

For research use only. We do not sell to patients.

BAY-298 Chemical Structure

BAY-298 Chemical Structure

CAS No. : 2471978-97-7

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5 mg USD 490 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels[1].

IC50 & Target

IC50: 185 nM (hLH), 46nM (rLH) and 78 nM (cLH)[1]

In Vivo

BAY-298 (oral; 4.5-72 mg/kg/day; for 8 days) dosedependently loweres serum estradiol levels in proestrus[1].
BAY-298 (iv of 0.5 mg/kg or po of 2 mg/kg) has t1/2s of 31 hours and 33 hours for iv and po. And the Cmaxs are 0.28 kg/L and 0.066 kg/L for iv and po[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Intact female rats[1]
Dosage: 4.5, 9, 18, 36, 72 mg/kg
Administration: Oral; for 8 days
Result: Dosedependently lowered serum estradiol levels in proestrus.
Animal Model: Female and male Wistar rats[1]
Dosage: 0.5 mg/kg of iv or 2 mg/kg of po
Administration: Iv or po
Result: Has t1/2s of 31 hours and 33 hours for iv and po. And the Cmaxs are 0.28 kg/L and 0.066 kg/L for iv and po.
Molecular Weight

473.93

Formula

C27H21ClFN3O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1[C@@H](C2=CC=C(Cl)C=C2)C3=C(N=CC=C3)CC1)NC4=CC=C(OC5=CC=C(F)C=C5)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (211.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.94%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1100 mL 10.5501 mL 21.1002 mL 52.7504 mL
5 mM 0.4220 mL 2.1100 mL 4.2200 mL 10.5501 mL
10 mM 0.2110 mL 1.0550 mL 2.1100 mL 5.2750 mL
15 mM 0.1407 mL 0.7033 mL 1.4067 mL 3.5167 mL
20 mM 0.1055 mL 0.5275 mL 1.0550 mL 2.6375 mL
25 mM 0.0844 mL 0.4220 mL 0.8440 mL 2.1100 mL
30 mM 0.0703 mL 0.3517 mL 0.7033 mL 1.7583 mL
40 mM 0.0528 mL 0.2638 mL 0.5275 mL 1.3188 mL
50 mM 0.0422 mL 0.2110 mL 0.4220 mL 1.0550 mL
60 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL
80 mM 0.0264 mL 0.1319 mL 0.2638 mL 0.6594 mL
100 mM 0.0211 mL 0.1055 mL 0.2110 mL 0.5275 mL
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BAY-298 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BAY-298
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