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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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

 

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
Purity & Documentation
References
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Y1693 Related Classifications

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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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