2. NF-κB Immunology/Inflammation Metabolic Enzyme/Protease
  3. RANKL/RANK Nuclear Factor of activated T Cells (NFAT) Cathepsin
  4. Y1693

Y1693 is an orally active RANKL inhibitor with a Kd 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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Y1693

Y1693 Chemical Structure

CAS No. : 2812381-74-9

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Y1693 Related Antibodies

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

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  • Purity & Documentation

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Description

Y1693 is an orally active RANKL inhibitor with a Kd 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[1][2].

IC50 & Target

Cathepsin E

 

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.

Y1693 Related Antibodies

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 AUC0-t T1/2 CL Cmax 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.
Molecular Weight

419.52

Formula

C28H25N3O
CAS No.
Appearance

Solid

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
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 : 25 mg/mL (59.59 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 2.3837 mL 11.9184 mL 23.8368 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 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.

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

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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 (5.96 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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 2.3837 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 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.

Keywords:

Y16932812381-74-9Y 1693Y-1693RANKL/RANKNuclear Factor of activated T Cells (NFAT)Cathepsinc-fos/NFATc1 signaling pathwaybone marrow-derived macrophagesRANKLTNFαosteoporosismouse bone marrow osteoclast precursor cellsperiodontal diseaseF-actin ringosteoclastRANKInhibitorinhibitorinhibit

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