| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H18N3O2PS |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Zharp2-1 is an orally effective RIPK2 inhibitor closely associated with inflammatory bowel disease (IBD). It blocks muramyl dipeptide (MDP)-induced growth of mononuclear cells and induces inflammatory cell factor infection, and it attenuates MDP-induced small inguinal peritonitis and ameliorates DNBS-induced large inguinal conjunctivitis[1]. It is supplied as a light yellow to yellow solid (C19H18N3O2PS, MW 383.40) at 99.10% purity.
Physical & Chemical Properties
| CAS Number | 2772600-18-5 |
|---|---|
| Molecular Formula | C19H18N3O2PS |
| Molecular Weight | 383.40 g/mol |
| Purity | 99.10% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=P(C)(C1=C(OC)C=C2N=CC=C(NC3=CC=C(SC=N4)C4=C3)C2=C1)C |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 5 mg/mL (13.04 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| 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. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 5 mg/mL (13.04 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
Pretreatment of THP-1 and iBMDM cells with Zharp2-1 for 2 h inhibits IL-6 and TNF-α release, which is induced for 12 h by 10 μg/mL MDP or 1 μg/mL L18-MDP[1]. In PBMCs, Zharp2-1 significantly inhibits MDP-induced cytokine release, with IC50 values 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 against DNBS-induced colon shortening, colon weight gain, and diarrhea. Zharp2-1 also significantly ameliorates colonic mucosal structural disruption, muscle thickening, and inflammatory infiltration[1].
Pharmacokinetic Analysis[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng·h/mL) | AUC (ng·h/mL) | Vd (L/kg) | Cl (mL/kg/min) | F (%) | |
| Mouse | iv | 2 | 1.2 | 2989 | 1.1 | 11.1 | |||
| po | 10 | 0.5 | 9610 | 19,236 | 129 | ||||
| Rat | iv | 2 | 1.7 | 7889 | 0.6 | 4.2 | |||
| po | 10 | 3.3 | 3323 | 18,803 | 48 | ||||
| Dog | iv | 1 | 2.1 | 1645 | 1.7 | 9.5 | |||
| po | 5 | 0.7 | 2192 | 10,800 | 131 |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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