| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
NLRP3 214 nM (IC50)
NP3-562 targets the NLRP3 inflammasome, a multiprotein complex that plays a critical role in the innate immune response. Activation of the NLRP3 inflammasome leads to the cleavage and secretion of pro-inflammatory cytokines like IL-1β and IL-18. By inhibiting NLRP3, NP3-562 blocks this inflammatory cascade. |
|---|---|
| ln Vitro |
In vitro, NP3-562 inhibits IL-1β release in nigericin-stimulated THP-1 cells with an IC50 of 66 nM and in human whole blood with an IC50 of 214 nM. These data demonstrate its potent anti-inflammatory activity in cellular and ex vivo models.
|
| ln Vivo |
In vivo, NP3-562 (30 mg/kg, oral) inhibits IL-1β release in a mouse acute peritonitis model. This confirms its oral activity and efficacy in a disease-relevant model.
|
| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for NP3-562 are not typically employed, as its target is a multiprotein complex. Instead, its activity is assessed by measuring its ability to inhibit IL-1β release in cell-based assays.
|
| Cell Assay |
In vitro cell-based assay protocols for NP3-562 involve stimulating immune cells, such as THP-1 macrophages, with an NLRP3 activator like nigericin in the presence of the compound. The amount of IL-1β released into the supernatant is then measured by ELISA.
|
| Animal Protocol |
In vivo animal experimental protocols for NP3-562 have been established in a mouse acute peritonitis model. Mice are administered NP3-562 orally (e.g., 30 mg/kg), followed by an intraperitoneal injection of an inflammatory stimulus. After a period of time, peritoneal lavage fluid is collected, and IL-1β levels are measured.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of NP3-562 indicate it is orally active. It is soluble in DMSO at 100 mg/mL. Specific PK parameters such as half-life and Cmax have not been reported.
|
| Toxicity/Toxicokinetics |
Toxicological data for NP3-562 are not available in the current literature. It is intended for research use only.
|
| References | |
| Additional Infomation |
NP3-562 is a research-grade compound used as a potent and orally active NLRP3 inhibitor for studying inflammation. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves inhibition of the NLRP3 inflammasome and subsequent IL-1β release. The compound is available exclusively for research purposes.
|
| CAS # |
2409825-32-5
|
|---|---|
| Appearance |
White to light yellow solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
|
|---|---|
| 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.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
