BAY-899

Name: BAY-899
Brand: MedChemExpress
SKU: HY-130248
Rating: 4.5 (1 reviews)

Cat. No.: HY-130248 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC₅₀s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels.

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

BAY-899 Chemical Structure

CAS No. : 2471967-92-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 111	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 111	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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(R)-BAY-899 Get quote

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Description

IC₅₀ & Target

IC50: 185 nM (hLH) and 46nM (rLH)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	10.6 μM Compound: 36; BAY-899	Inhibition of human ERG expressed in HEK293 cells at holding potential -80 mV by whole-cell voltage-clamp method Inhibition of human ERG expressed in HEK293 cells at holding potential -80 mV by whole-cell voltage-clamp method	[PMID: 31670515]

In Vivo

BAY-899 (oral; 12.5 mg/kg/day; for 8 days) shows an efficiency to reduce serum estradiol levels in intact female rats^[1].
BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t_1/2 of 11 hours and 12 hours for iv and po. And the C_max is 0.97 kg/L and 0.24 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:	12.5 mg/kg
Administration:	Oral; for 8 days
Result:	Showed an efficiency to reduce serum estradiol levels.

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 t_1/2s of 11 hours and 12 hours for iv and po. And the C_maxs are 0.97 kg/L and 0.24 kg/L for iv and po.

Molecular Weight

459.45

Formula

C₂₅H₁₉F₂N₅O₂

CAS No.

2471967-92-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@H](C2=CC=C(F)C=C2)C3=C(N=CC=C3)CC1)NC4=CN=C(OC5=CC=C(F)C=C5)N=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 : 130 mg/mL (282.95 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	2.1765 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

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.5 mg/mL (7.62 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.5 mg/mL (7.62 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3.5 mg/mL (7.62 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 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 (35.0 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)

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: 99.93%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (247 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1765 mL	10.8826 mL	21.7652 mL	54.4129 mL
	5 mM	0.4353 mL	2.1765 mL	4.3530 mL	10.8826 mL
	10 mM	0.2177 mL	1.0883 mL	2.1765 mL	5.4413 mL
	15 mM	0.1451 mL	0.7255 mL	1.4510 mL	3.6275 mL
	20 mM	0.1088 mL	0.5441 mL	1.0883 mL	2.7206 mL
	25 mM	0.0871 mL	0.4353 mL	0.8706 mL	2.1765 mL
	30 mM	0.0726 mL	0.3628 mL	0.7255 mL	1.8138 mL
	40 mM	0.0544 mL	0.2721 mL	0.5441 mL	1.3603 mL
	50 mM	0.0435 mL	0.2177 mL	0.4353 mL	1.0883 mL
	60 mM	0.0363 mL	0.1814 mL	0.3628 mL	0.9069 mL
	80 mM	0.0272 mL	0.1360 mL	0.2721 mL	0.6802 mL
	100 mM	0.0218 mL	0.1088 mL	0.2177 mL	0.5441 mL

BAY-899 Related Classifications

Endocrinology

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.

Keywords:

BAY-8992471967-92-5BAY899BAY 899GnRH ReceptorGonadotropin releasing hormone receptorGNRHRInhibitorinhibitorinhibit

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