| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SH494 (0.01-1 μM; 7 days) effectively inhibited RANKL-induced differentiation of mouse bone marrow macrophages (BMM) into osteoclasts, with an IC50 of 8.4 nM. At concentrations ≥0.1 μM, the process was completely inhibited after 7 days of treatment [1]. SH494 (0.01-1 μM; 7 days) dose-dependently inhibited the formation of F-actin loops in RANKL-induced mouse bone marrow macrophages (BMM) [1]. SH494 (0.01-1 μM; 1-5 days) dose- and time-dependently downregulated the mRNA expression of key osteoclastogenesis genes in RANKL- and M-CSF-treated mouse bone marrow macrophages (BMM) [1]. SH494 (0.01–1 μM; 72 h) dose-dependently inhibited the protein expression of key osteoclastogenesis markers (c-Fos, Ctsk, Mmp9) in mouse bone marrow-derived macrophages (BMMs) [1]. SH494 (1 μM; 5–30 min) inhibited RANKL-induced p38 MAPK phosphorylation in mouse bone marrow macrophages (BMMs) at 5, 10, and 30 min after RANKL stimulation [1]. SH494 (0.01–1 μM; 48–72 h) reduced RANKL-induced ROS accumulation in mouse bone marrow macrophages (BMMs) and restored their mitochondrial membrane potential after 48 h; at the same time, it activated the Nrf2 pathway by upregulating the expression of Cat, Gclc, and HO-1 and increasing the nuclear localization of Nrf2 [1].
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| ln Vivo |
SH494 (1–5 mg/kg; intraperitoneal injection; once daily; 6 weeks) can prevent ovariectomy-induced bone loss in mice in a dose-dependent manner [1].
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| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: Mouse bone marrow-derived macrophages (BMM) Tested Concentrations: 0.01 μM (48 hours), 0.1 μM (48 hours), 1 μM (48 hours; 1, 3, 5 days) Incubation Duration: 48 hours (concentration-dependent analysis); 1, 3, 5 days (time course of 1 μM SH494) Experimental Results: After 48 hours, the mRNA expression of key osteoclastogenesis markers Nfatc1, Trap, Ctsk, Mmp9, and c-Fos was downregulated in a dose-dependent manner. Over a 5-day time course, 1 μM SH494 eliminated the RANKL-induced upregulation of Nfatc1, Trap, Ctsk, and c-Fos throughout the differentiation process. Western Blot Analysis [1] Cell Types: Mouse bone marrow-derived macrophages (BMM) Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM Incubation Duration: 72 hours Experimental Results: The protein levels of c-Fos, Ctsk and Mmp9 in RANKL-stimulated BMM decreased in a dose-dependent manner. Western Blot Analysis [1] Cell Types: Mouse bone marrow-derived macrophages (BMM) Tested Concentrations: 1 μM Incubation Duration: Pretreatment followed by incubation with RANKL for 5, 10, and 30 minutes Experimental Results: Significantly inhibited RANKL-induced p38 phosphorylation at all test time points. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (8-week-old females; bilateral ovariectomy-induced osteoporosis) [1]
Doses: 1 mg/kg; 5 mg/kg Route of Administration: Intraperitoneal injection; once daily for 6 weeks Experimental Results: Compared with ovariectomized mice treated with the vector, the 5 mg/kg dose group showed a 40.66% increase in bone volume fraction (BV/TV), a 28.35% increase in trabecular bone number (Tb.N), and a 33.43% increase in bone surface density (BS/TV). The dose-dependent prevention of ovariectomy-induced bone microstructural deterioration was achieved, with the 5 mg/kg dose group showing comparable improvement in Tb.N and BS/TV to the positive control teriparatide. The treatment group preserved trabecular bone structure and reduced osteoclast number. No systemic or organ-specific toxicity was observed, body weight remained stable, and the histology of major organs was normal. |
| References |
| Molecular Formula |
C31H34N4O2
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|---|---|
| Molecular Weight |
494.63
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
C[C@]12[C@]([H])([C@@]3(CCC4=CC(CC[C@@]4(C3=CC2)C)=O)[H])CC(C1=NC5=NC=NN65)=C6C7=CC=C(C=C7)OCCC
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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 | 2.0217 mL | 10.1086 mL | 20.2171 mL | |
| 5 mM | 0.4043 mL | 2.0217 mL | 4.0434 mL | |
| 10 mM | 0.2022 mL | 1.0109 mL | 2.0217 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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