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MedChemExpress - Model Zharp2-1 - ...

MedChemExpress - Model Zharp2-1 - 2772600-18-5

Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis[1].

Zharp2-1

MCE China：Zharp2-1

Brand：MedChemExpress (MCE)

Cat. No.HY-155782

CAS：2772600-18-5

Purity：99.59%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis.

In Vitro：Zharp2-1 pretreats THP-1 and iBMDM cells for 2 h, and inhibits the release of IL-6 and TNF-α induced by 10 μg/mL MDP or 1 μg/mL L18-MDP for 12 h[1].Zharp2-1 significantly inhibits MDP-induced cytokine release in PBMCs, with an IC50 of 0.8 nM for IL-8, 8.7 nM for IL-6 and 11.9 nM for TNF-α[1].

In Vivo：Zharp2-1 (15 mg/kg; gavage; once daily for 6 days) protects rats from DNBS-induced colon shortening and colon weight gain, protects rats against DNBS-induced diarrhea. Zharp2-1 significantly ameliorates colonic mucosal structural disruption, muscle thickening and inflammatory infiltration[1].Pharmacokinetic Analysis[1] RouteDose (mg/kg)T1/2 (h)Tmax (h)Cmax (ng·h/mL)AUC (ng·h/mL)Vd (L/kg)Cl (mL/kg/min)F (%) Mouseiv21.2 29891.111.1 po10 0.5961019,236 129 Rativ21.7 78890.64.2 po10 3.3332318,803 48 Dogiv12.1 16451.79.5 po5 0.7219210,800 131

IC50 & Target：RIPK2[1] In Vitro Zharp2-1 pretreats THP-1 and iBMDM cells for 2 h, and inhibits the release of IL-6 and TNF-α induced by 10 μg/mL MDP or 1 μg/mL L18-MDP for 12 h[1].Zharp2-1 significantly inhibits MDP-induced cytokine release in PBMCs, with an IC50 of 0.8 nM for IL-8, 8.7 nM for IL-6 and 11.9 nM for TNF-α[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Zharp2-1 Related Antibodies

References：

[1]. Lai Y, et al. Discovery of a novel RIPK2 inhibitor for the treatment of inflammatory bowel disease. Biochem Pharmacol. 2023 Aug;214:115647. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。