| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
Y1693 (0.1-10 μM; 5-6 days) effectively inhibited RANKL-induced osteoclastogenesis in bone marrow monocytes (BMMs), with an IC50 of 0.52 μM. The inhibition rate was 89.3% at 1 μM and 45.9% at 0.1 μM [1]. Y1693 (1-10 μM; 3 days) showed no cytotoxicity to BMMs at concentrations up to 10 μM [1]. Y1693 (0.1-5 μM; 5-6 days) inhibited RANKL-induced F-actin ring formation in BMM-derived osteoclasts in vitro in a dose-dependent manner [1]. Y1693 (0.5-5 μM; 3 days) downregulated the mRNA expression of TRAP, cathepsin K, c-fos, and NFATc1 in RANKL-stimulated BMM cells in a dose-dependent manner [1]. Y1693 (1–10 μM; 3 days) dose-dependently inhibited the protein expression of c-fos and NFATc1 in RANKL-stimulated BMM cells [1]. Y1693 (0.1–5 μM; 2 days) dose-dependently inhibited RANKL-induced bone resorption of bovine femoral sections by mature osteoclasts, with almost complete inhibition at 5 μM [1].
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| ln Vivo |
Y1693 (20-60 mg/kg; oral administration; once daily, 5 times a week; for 28 days) restored bone mineral density by 23.4% in ovariectomized osteoporotic mice and improved bone loss[1]. Y1693 (20 mg/kg; intraperitoneal injection; once daily; for 28 days) increased alveolar bone mass by 60.7% and bone volume by 51.9% in mice, while also improving ligation-induced periodontal bone loss in mice[1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Bone marrow-derived macrophages (BMM) Tested Concentrations: 1 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 3 days Experimental Results: No cytotoxicity was observed in BMM at concentrations up to 10 μM. Relative cell viability remained above 1.5-fold at all test concentrations (similar to the untreated control group). Real-time quantitative PCR [1] Cell Types: Bone marrow-derived macrophages (BMM) Tested Concentrations: 0.5 μM, 1 μM, 2.5 μM, 5 μM Incubation Duration: 3 days Experimental Results: Dose-dependently reduced the upregulation of RANKL-induced osteoclast marker genes. At a concentration of 5 μM, the mRNA levels of TRAP, cathepsin K, c-fos, and NFATc1 were suppressed to near basal (unstimulated) levels. Significant inhibitory effects were also observed at concentrations as low as 0.5 μM. Western Blot Analysis [1] Cell Types: Bone marrow-derived macrophages (BMM) Tested Concentrations: 1 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 3 days Experimental Results: c-fos and NFATc1 protein expression decreased in a dose-dependent manner. Protein levels gradually decreased as the concentration increased from 1 μM to 10 μM. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 osteoporotic mice (8-week-old females; ovariectomy-induced osteoporosis)[1]
Doses: 20 mg/kg; 60 mg/kg Route of Administration: Oral; once daily, 5 times a week; for 28 days Experimental Results: Compared with ovariectomized control mice, bone mineral density increased by 23.4%. Improved osteoporosis-related bone loss. Animal/Disease Models:BALB/c mouse periodontitis model (8-week-old males; ligation-induced periodontitis) [1] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection; once daily for 28 days Experimental Results: Compared with the ligation-induced periodontitis control group, alveolar bone mass increased by 60.7%. Bone volume increased by 51.9% compared with the ligation-induced periodontitis control group. Vertical alveolar bone mass of M2-M3 increased by 67.0% compared with the ligation-induced periodontitis control group. Alveolar bone structure was preserved. |
| References |
| Molecular Formula |
C28H25N3O
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|---|---|
| Molecular Weight |
419.52
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| CAS # |
2812381-74-9
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| Appearance |
White to off-white solid
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| SMILES |
O=C(C1=CC2=C(NC3=C2C=CC=C3)C(CCC4=CC=CC=C4)=N1)NC5=C(C)C=CC=C5C
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2384 mL | 1.1918 mL | 2.3837 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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