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RI-962

Catalog No. T73493   CAS 2763831-53-2

RI-962 is a potent and selective inhibitor of receptor-interacting protein kinase 1 (RIPK1), exhibiting an IC50 of 35.0 nM. It is utilized for the investigation of nervous system disorders and inflammatory diseases [1].

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RI-962 Chemical Structure
RI-962, CAS 2763831-53-2
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RI-962 is a potent and selective inhibitor of receptor-interacting protein kinase 1 (RIPK1), exhibiting an IC50 of 35.0 nM. It is utilized for the investigation of nervous system disorders and inflammatory diseases [1].
In vitro RI-962 exhibits a strong inhibitory activity against RIPK1, demonstrated by an IC50 of 35.0 nM [1]. Furthermore, RI-962 offers a protective effect against necroptotic cell death, with EC50 values of 10.0 nM for HT29 cells, 4.2 nM for L929 cells, 11.4 nM for J774A.1 cells, and 17.8 nM for U937 cells [1]. At concentrations ranging from 0-100 μM over 24 hours, RI-962 safeguards cells from TSZ-induced necroptosis by impeding RIPK1's kinase activity [1].
In vivo RI-962, administered intraperitoneally (i.p.) at a dosage of 40 mg/kg once daily for 10 days, alleviates TNFα-induced systemic inflammatory response syndrome (SIRS) and mitigates inflammation in acute DSS-induced colitis [1]. The pharmacokinetic profile of RI-962 in rats, following intravenous (i.v.), intraperitoneal (i.p.), and oral (p.o.) administration at doses of 5 and 20 mg/kg, includes a half-life (T1/2) of 2.1±0.2 hours (i.v., 5 mg/kg), 1.3±0.2 hours (p.o., 20 mg/kg), and 8.5±1.6 hours (i.p., 20 mg/kg). The peak plasma concentration (Cmax) reached 12170.4±1198.5 ng/mL (i.v.), 674.2±424.7 ng/mL (p.o.), and 3603.3±693.3 ng/mL (i.p.). The area under the concentration-time curve from zero to the last observed time point (AUC 0–t) and to infinity (AUC 0–∞) showed comparable values. The volume of distribution at steady-state (Vss) was recorded for i.v. administration at 0.4±0.1 L/kg, and the mean residence time (MRT 0–∞) varied across administration routes [1].
Molecular Weight 480.56
Formula C28H28N6O2
CAS No. 2763831-53-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

RI-962 2763831-53-2 Apoptosis NF-Κb RIP kinase inhibitor inhibit

 

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