Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
NLRP3 inflammasome[1]
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ln Vitro |
In THP-M cells, NLRP3-IN-12 (Compound 6E) (0.5-2 μM; 1 h pretreatment) suppresses cleaved caspase-1 and IL-1β production when triggered by LPS and ATP [1]. In THP-M cells, NLRP3-IN-12 (2 μM) prevents GSDMD-mediated apoptosis [1]. In human and rat liver microsomes, the half-lives (T1/2) of NLRP3-IN-12 (1 μM) are 53.4 and 31.8 minutes, respectively[1].
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ln Vivo |
In mice, NLRP3-IN-12 (Compound 6E) (5–10 mg/kg; i.p. daily for 10 days) reduces the severity of DSS-induced colitis [1]. In rats, NLRP3-IN-12 (20 mg/kg; iv) has a half-life (T1/2) of 6.64 hours, an elimination rate constant (Kel) of 0.107 hours, and a clearance rate (CL) of 105 mL/kg/min. At steady state, the apparent volume of distribution (Vdss) is 23.1 L/kg[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: THP-M cells Tested Concentrations: 0.5, 1, 2 μM Incubation Duration: Pretreated for 1 h, then stimulated with LPS(1 μg/mL) for 4.5 h, and ATP(5 mM) for 0.5 h. Experimental Results: decreased the secretion of IL-1β and caspase-1. Had no effect on the levels of NLRP3, pro-IL-1β, ASC, pro-caspase 1, p65, p-p65, IκBα, and p- IκBα. |
Animal Protocol |
Animal/Disease Models: C57BL/6 mice were induced acute colitis by drinking 3% DSS (dextran sulfate sodium)[1]
Doses: 5, 10 mg/kg Route of Administration: intraperitoneal (ip)injection daily for 10 days in aqueous solution containing DMSO/0.5% CMC- Na/normal saline Experimental Results: Attenuated DSS-induced weight loss, loose stools, bloody stools, shortened colons, increased disease activity index score, and lower survival rate. |
References |
[1]. Pang L, et, al. Development of novel oridonin analogs as specifically targeted NLRP3 inflammasome inhibitors for the treatment of dextran sulfate sodium-induced colitis. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114919.
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Molecular Formula |
C27H32CLNO7
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Molecular Weight |
518.00
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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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9305 mL | 9.6525 mL | 19.3050 mL | |
5 mM | 0.3861 mL | 1.9305 mL | 3.8610 mL | |
10 mM | 0.1931 mL | 0.9653 mL | 1.9305 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.