NLRP3-IN-10 NEW
| Price | $39 | $64 | $128 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: NLRP3-IN-10 | CAS No.: 2641826-39-1 |
| Purity: 99.63% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | NLRP3-IN-10 |
| Description | NLRP3-IN-10 (ZVN26391) is a potent NLRP3 inhibitor. NLRP3-IN-10 inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 attenuates ASC speck formation, leading to suppress activation of NLRP3 inflammasome. |
| In vitro | NLRP3-IN-10 (compound 14c) significantly inhibits NLRP3 inflammasome activation in THP-1 cells by LPS-MSU, demonstrating dose-dependent efficacy at 0.4-6.4 μM over 40 minutes. It is non-toxic to THP-1 cells at 0.1-6.4 μM after 1.5 hours and prevents Nigericin-induced pyroptosis at 0.1 and 0.4 μM. The compound reduces caspase-1 p20 and IL-1β production dose-dependently at 0.1, 0.2, and 0.4 μM, and decreases LPS-induced TNF-α production at 3 and 5 μM. NLRP3-IN-10 also reduces ASC specks formation at 0.2 and 0.8 μM, indicating interruption of ASC oligomerization. Furthermore, it inhibits LPS-induced NLRP3 priming by directly interacting with NLRP3 at 1, 10, and 100 μM, demonstrating potential in regulating both priming and activation steps in the NLRP3 inflammasome pathway. |
| In vivo | NLRP3-IN-10 (compound 14c), administered via a single intravenous (i.v.) dose of 10 mg/kg, effectively reduced peritoneal neutrophil influx and IL-1β levels in the spleen in a LPS-primed mouse model with MSU-induced peritonitis. Additionally, oral administration of NLRP3-IN-10 at doses of 10, 30, and 90 mg/kg demonstrated very low systemic exposure (14.6 to 23.53 μg·h/L), limited bioavailability (2.47 to 13.79%), and high plasma clearance rates (2201.58 to 5551.12 L/h/kg), indicating significant challenges in its pharmacokinetic profile when administered orally. Pharmacokinetic data revealed an area under the curve (AUC) ranging from 14.60 to 23.53 μg·h/L, clearance (CL) rates between 2201.58 and 5551.12 L/h/kg, and maximal concentration (Cmax) values from 3.35 to 81.97 μg/L across different administration routes and dosages. The study was conducted on 7-week-old male C57BL/6J mice induced with MSU-induced peritonitis and primed with LPS (1 mg/kg, i.p.), showing a notable reduction in spleen IL-1β release and peritoneal neutrophil influx following a 6-hour treatment with a 10 mg/kg intravenous dose of NLRP3-IN-10, when compared to the control group. |
| Storage | Shipping with blue ice. |
| Solubility Information | DMSO : 4.4 mg/mL (12.05 mM) |
| Keywords | NLRP3-IN-10 | ZVN 26391 | ZVN-26391 |
| Inhibitors Related | BAL-0028 | Dapansutrile | NOD-IN-1 | CY-09 | MCC950 sodium | Imperatorin | Asymmetric dimethylarginine | NLRP3-IN-2 | Bergenin | NLRP3-IN-9 | INF39 | Selnoflast |
| Related Compound Libraries | NF-κB Signaling Compound Library | Bioactive Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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