| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
KW-8232 free base targets PGE2 biosynthesis, reducing its production. PGE2 is a key mediator of bone resorption and inflammation. By reducing PGE2 biosynthesis, the compound exerts anti-osteoporotic effects. Additionally, KW-8232 exhibits antiviral activity against SARS-CoV-2.
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| ln Vitro |
KW-8232 is a medication that prevents osteoporosis. In mouse osteoblasts, KW-8232 lowers PGE2 biosynthesis [1]. KW-8232 exhibits antiviral efficacy against SARS-CoV-2 (EC50 ~1.2 μM) [2].
KW-8232 free base demonstrates in vitro activity by reducing PGE2 biosynthesis in mouse osteoblasts. It exhibits antiviral efficacy against SARS-CoV-2 with an EC₅0 of approximately 1.2 uM. The compound shows potential for both bone and antiviral applications. Purity is typically >98%. |
| ln Vivo |
In immobilized rat legs, KW-8232 (3, 10, 30 mg/kg, oral) can effectively increase femoral bone mineral density (BMD) and influence abnormal bone turnover brought on by immobilization. At only 30 mg/kg, KW-8232 dramatically decreased the amount of calcium excreted in the urine of neurectomized rats. It also significantly decreased the amount of pyridinoline and deoxypyridinoline excreted in the urine, which are the main constituents of neurectomized rats. indicators of mouse bone resorption. By controlling PGE2 production, KW-8232 may be able to reduce prostaglandin (PG)-stimulated bone resorption and thereby inhibit bone loss [1].
In vivo, KW-8232 free base is an orally active anti-osteoporotic agent. Oral administration has been studied for its effects on bone metabolism and PGE2 reduction. The compound's antiviral efficacy against SARS-CoV-2 suggests potential for in vivo antiviral applications. Further in vivo studies are needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
In vitro enzyme/activity assays for KW-8232 free base typically involve measuring PGE2 biosynthesis in cell-based systems such as mouse osteoblasts or other PGE2-producing cells. Cells are treated with varying concentrations of the compound, and PGE2 levels in the culture medium are measured by ELISA. Antiviral activity against SARS-CoV-2 is assessed using viral replication assays with EC₅0 determination.
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| Cell Assay |
In vitro cellular assays for KW-8232 free base involve treating osteoblast cell lines or PGE2-producing cells with varying concentrations of the compound (typically 0.01-100 microM range) for 24-72 hours. Readouts include PGE2 levels measured by ELISA, assessment of cell viability, and evaluation of bone-related markers. Antiviral assays using SARS-CoV-2-infected cells assess viral replication inhibition.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (5 weeks old) [1].
Doses: 1, 3, 10 and 30 mg/kg. Doses: Take orally one time/day starting 1 day before neurectomy for 28 days. Experimental Results: Urinary calcium excretion in neurectomized rats was diminished only at 30 mg/kg. In vivo animal studies for KW-8232 free base typically employ rodent models of osteoporosis or bone loss. Animals are administered the compound via oral gavage at various doses. Endpoints include assessment of bone mineral density, bone turnover markers, PGE2 levels, and histomorphometric analysis of bone tissue. Antiviral efficacy would be assessed in appropriate infection models. |
| ADME/Pharmacokinetics |
KW-8232 free base is orally active with favorable pharmacokinetic properties. Following oral administration, the compound achieves appropriate exposure for target engagement. PK parameters including half-life, Cmax, Tmax, and AUC are determined via LC-MS/MS analysis. The compound is typically stored at -20degC (powder form for 3 years, solution for 6 months).
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| Toxicity/Toxicokinetics |
Toxicological data for KW-8232 free base is limited. As a research compound, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. The compound is for research use only and not for human therapeutic use. Comprehensive toxicology studies would be required for clinical development.
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| References | |
| Additional Infomation |
KW-8232 free base (CAS# 170365-25-0) is an orally active anti-osteoporotic agent that reduces PGE2 biosynthesis. It also exhibits antiviral efficacy against SARS-CoV-2 (EC₅0 ~1.2 uM). The compound is not approved for clinical use and is for research purposes only. It is typically stored at -20degC. Not for human therapeutic use.
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| Molecular Formula |
C36H37CLN4O3
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|---|---|
| Molecular Weight |
609.156987905502
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| Exact Mass |
608.255
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| CAS # |
170365-25-0
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| Related CAS # |
KW-8232;217813-15-5
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| PubChem CID |
3025960
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| Appearance |
Off-white to pink solid powder
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| LogP |
6.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
44
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| Complexity |
893
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC=CC=1N1CCN(C(C2=C(C3C=CC=CC=3N2CCN(C)C)C(C2C=CC(=CC=2)O)C2C=CC(=CC=2)O)=O)CC1
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| InChi Key |
HESAJCAYRSKRSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H37ClN4O3/c1-38(2)19-24-41-31-9-5-3-7-29(31)34(33(25-11-15-27(42)16-12-25)26-13-17-28(43)18-14-26)35(41)36(44)40-22-20-39(21-23-40)32-10-6-4-8-30(32)37/h3-18,33,42-43H,19-24H2,1-2H3
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| Chemical Name |
[3-[bis(4-hydroxyphenyl)methyl]-1-[2-(dimethylamino)ethyl]indol-2-yl]-[4-(2-chlorophenyl)piperazin-1-yl]methanone
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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 | 1.6416 mL | 8.2080 mL | 16.4160 mL | |
| 5 mM | 0.3283 mL | 1.6416 mL | 3.2832 mL | |
| 10 mM | 0.1642 mL | 0.8208 mL | 1.6416 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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