| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
G721-0282 (5-20 μM) can inhibit lipopolysaccharide (LPS)-induced neuroinflammation in BV-2 cells, including NO production, expression of pro-inflammatory cytokines, and levels of inflammatory proteins [1]. G721-0282 (20 μM) exerts anti-inflammatory effects on BV-2 cells through CHI3L1 [1]. G721-0282 (10-50 μM, 24-72 h) inhibits the proliferation of MG63 and U2OS cells in a dose- and time-dependent manner [2]. G721-0282 (0-50 μM, 24 h) can arrest the cell cycle of MG63 and U2OS cells and induce apoptosis by downregulating the levels of anti-apoptotic proteins and upregulating the levels of pro-apoptotic proteins [2]. G721-0282 (0-50 μM, 12-48 h) significantly inhibited the migration and invasion of MG63 and U2OS cells by suppressing the STAT3 signaling pathway [2]. G721-0282 (2-4 weeks) inhibited the colony-forming ability of osteosarcoma (OS) cells in soft agar [2]. G721-0282 (0-50 μM, 24 h) reduced the levels of MMP2 and MMP9 [2].
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| ln Vivo |
G721-0282 (2.5 and 5 mg/kg; orally; twice weekly for 4 weeks) significantly reduced anxiety-like behavior and suppressed neuroinflammation in male BALB/c mice induced by chronic unpredictable mild stress (CUMS) [1]. G721-0282 (18.9 mg/kg; intraperitoneally; twice weekly for 35 days) showed significant antitumor activity in male BALB/c athymic nude mice carrying MG63 tumors [2].
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| Cell Assay |
Western Blot Analysis [2]
Cell Types: MG63 and U2OS cells Tested Concentrations: 10, 30 and 50 μM Incubation Duration: 24 hours Experimental Results: Significantly reduced the levels of Cyclin D1, cdk4, cdk6, ERK1/2, JNK, p38, Src, STAT3, Survivin and Bcl-2, and increased the levels of cleaved PARP and cleaved caspase-3. |
| Animal Protocol |
Animal/Disease Models:Male BALB/c mice (8 weeks old) induced by chronic unpredictable stress (CUMS) [1]
Doses: 2.5 and 5 mg/kg Route of Administration: Oral (po); twice weekly for 4 weeks Experimental Results: Significantly reduced anxiety behavior in mice. Significantly reduced the expression of inflammatory proteins, including iNOS, COX-2, IBA-1, p65, p50, and p-IκBα. Reduced the expression of inflammatory factors, including TNF-α, IL-1β, and IL-6. Inhibited the NF-κB signaling pathway. Reduced the expression of CUMS-induced CHI3L1 and IGFBP3. Animal/Disease Models:1 × 10⁸ MG63 cells were injected into male BALB/c athymic nude mice (6 weeks) [2] Doses: 18.9 mg/kg Route of Administration: Intraperitoneal injection (ip); twice a week for 35 days Experimental Results: Significantly inhibited tumor volume and weight. Reduced the expression of CHI3L1, PCNA, Cyclin D1, and p-STAT3 in tumor tissue. |
| References |
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| Molecular Formula |
C18H24N4O3S
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|---|---|
| Molecular Weight |
376.47
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| CAS # |
946378-12-7
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| Appearance |
White to off-white solid
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| SMILES |
O=C1C2=C(C(CCCC)=CN=C2N(C)C(N1C)=O)SCC(NCC=C)=O
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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) |
DMSO : ~5.83 mg/mL (~15.49 mM; with sonication)
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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 | 2.6563 mL | 13.2813 mL | 26.5625 mL | |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3125 mL | |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6563 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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