Art. -Nr.: HY-182757

Y1693

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Y1693 is an orally active RANKL inhibitor with a K_d of 5.03 μM for hRANKL. Y1693 inhibits the activation of the downstream c-fos/NFATc1 signaling pathway by blocking its interaction with RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation and bone resorptive activity, while downregulating the mRNA and protein expressions of TRAP, cathepsin K, c-fos and NFATc1. Y1693 shows no obvious cytotoxicity to bone marrow-derived macrophages and osteoclast precursor cells, and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research related to osteoporosis and periodontal diseases.

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Reinheit: 99.91%
CAS. Nr.: 2812381-74-9
Formel: C₂₈H₂₅N₃O
Molecular Weight:419.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Y1693 Chemical Structure

CAS. Nr.: 2812381-74-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Cathepsin E

Alle Cathepsin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BMDM	IC₅₀	0.52 μM Compound: 1; Y1693	Anti-osteoporosis activity C57/BL6 mouse bone marrow macrophage cells assessed as inhibition of RANKL-induced osteoclastogenesis measured after 5 to 6 days in presence of M-CSF by DAPI staining analysis Anti-osteoporosis activity C57/BL6 mouse bone marrow macrophage cells assessed as inhibition of RANKL-induced osteoclastogenesis measured after 5 to 6 days in presence of M-CSF by DAPI staining analysis	[PMID: 35960655]

In Vitro

Y1693 (0.1-10 μM; 5-6 day) potently inhibits RANKL-induced osteoclastogenesis in BMMs with an IC₅₀ of 0.52 μM, achieving 89.3% inhibition at 1 μM and 45.9% inhibition at 0.1 μM^[1].
Y1693 (1-10 μM; 3 day) is non-cytotoxic to BMMs at concentrations up to 10 μM^[1].
Y1693 (0.1-5 μM; 5-6 day) inhibits RANKL-induced F-actin ring formation in BMM-derived osteoclasts in vitro in a dose-dependent manner^[1].
Y1693 (0.5-5 μM; 3 day) dose-dependently downregulates the mRNA expression of TRAP, cathepsin K, c-fos, and NFATc1 in RANKL-stimulated BMMs^[1].
Y1693 (1-10 μM; 3 day) dose-dependently inhibits the protein expression of c-fos and NFATc1 in RANKL-stimulated BMMs^[1].
Y1693 (0.1-5 μM; 2 day) dose-dependently inhibits RANKL-induced bone resorption by mature osteoclasts on bovine femur bone slices, with nearly complete inhibition at 5 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:

bone marrow-derived macrophages (BMMs)
Concentration:

1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:

3 day
Result:

Showed no cytotoxicity to BMMs at concentrations up to 10 μM.
Maintained relative cell viability above 1.5-fold (similar to untreated controls) across all tested concentrations.

Real Time qPCR^[1]

Cell Line:

bone marrow-derived macrophages (BMMs)
Concentration:

0.5 μM, 1 μM, 2.5 μM, 5 μM
Incubation Time:

3 day
Result:

Dose-dependently reduced the RANKL-induced upregulation of osteoclast marker genes.
Suppressed TRAP, cathepsin K, c-fos, and NFATc1 mRNA levels to near basal (unstimulated) levels at 5 μM.
Exhibited significant inhibition at concentrations as low as 0.5 μM.

Western Blot Analysis^[1]

Cell Line:

bone marrow-derived macrophages (BMMs)
Concentration:

1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:

3 day
Result:

Reduced the protein expression of c-fos and NFATc1 in a dose-dependent manner.
Showed decreasing protein levels as concentration increased from 1 μM to 10 μM.

Parmacokinetics

Species	Dose	Route	AUC_0-t	T_1/2	CL	C_max	F
Rat^[1]	3 mg/kg	i.v.	2710 ng·h/mL	5.1 h	18.6 mL/min/kg	/	/
Rat^[1]	5 mg/kg	p.o.	223 ng·h/mL	2.0 h	/	48.1 ng/mL	4.9 %

In Vivo

Y1693 (20-60 mg/kg; p.o.; once daily 5×/week; 28 days) produces a 23.4% recovery of bone mineral density and ameliorates bone loss in ovariectomized mice with osteoporosis^[1].
Y1693 (20 mg/kg; i.p.; daily; 28 days) increases alveolar bone mass by 60.7%, bone volume by 51.9%, while ameliorating ligature-induced periodontal bone loss in mice^[1].

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

Animal Model:

C57BL/6 mice with Osteoporosis (8-week-old female; ovariectomy-induced osteoporosis)^[1]
Dosage:

20 mg/kg; 60 mg/kg
Administration:

p.o.; once daily 5×/week; 28 days
Result:

Increased bone mineral density by 23.4% compared to ovariectomized control mice.
Ameliorated osteoporosis-related bone loss.

Animal Model:

BALB/C mice with Periodontal disease (8-week-old male; ligature-induced periodontal disease)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; daily; 28 days
Result:

Increased alveolar bone mass by 60.7% compared to ligature-induced periodontal disease control mice.
Increased bone volume by 51.9% compared to ligature-induced periodontal disease control mice.
Increased vertical bone remaining at M2-M3 by 67.0% compared to ligature-induced periodontal disease control mice.
Preserved alveolar bone structure.

Chemical Information

CAS. Nr. 2812381-74-9
Appearance Solid
Molecular Weight 419.52
Formel C₂₈H₂₅N₃O
Color White to off-white
SMILES

O=C(C1=CC2=C(NC3=C2C=CC=C3)C(CCC4=CC=CC=C4)=N1)NC5=C(C)C=CC=C5C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (59.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3837 mL

11.9184 mL

23.8368 mL

5 mM

0.4767 mL

2.3837 mL

4.7674 mL

10 mM

0.2384 mL

1.1918 mL

2.3837 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.96 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yang K, et al. Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-κB Ligand. J Med Chem. 2022;65(16):10992-11009. [Content Brief]

[2]. Zhang Xiaofei, et al. A class of 3-amido-β-carboline compounds, their preparation method and use. CN116332929A. 2021-12-23.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.3837 mL	11.9184 mL	23.8368 mL	59.5919 mL
	5 mM	0.4767 mL	2.3837 mL	4.7674 mL	11.9184 mL
	10 mM	0.2384 mL	1.1918 mL	2.3837 mL	5.9592 mL
	15 mM	0.1589 mL	0.7946 mL	1.5891 mL	3.9728 mL
	20 mM	0.1192 mL	0.5959 mL	1.1918 mL	2.9796 mL
	25 mM	0.0953 mL	0.4767 mL	0.9535 mL	2.3837 mL
	30 mM	0.0795 mL	0.3973 mL	0.7946 mL	1.9864 mL
	40 mM	0.0596 mL	0.2980 mL	0.5959 mL	1.4898 mL
	50 mM	0.0477 mL	0.2384 mL	0.4767 mL	1.1918 mL

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Y1693

Orally Active Compound Library

Angiogenesis-Related Compound Library

Protein-protein Interaction Inhibitor Library

Osteogenesis Compound Library

Protease Inhibitor Library

Macrophage Related Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Aging Compound Library

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Y1693

Orally Active Compound Library

Angiogenesis-Related Compound Library

Protein-protein Interaction Inhibitor Library

Osteogenesis Compound Library

Protease Inhibitor Library

Macrophage Related Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Aging Compound Library

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Y1693 Related Classifications

HY-182757 Related Classifications