| Identification | Back Directory | [Name]
Benzamide, 4-[5-[(4-cyclopropyl-1H-indazol-5-yl)amino]-1-methyl-1H-1,2,4-triazol-3-yl]-N-(2,2-difluoroethyl)- | [CAS]
2365193-22-0 | [Synonyms]
RXC-007
RXC-007/zelasudil
Benzamide, 4-[5-[(4-cyclopropyl-1H-indazol-5-yl)amino]-1-methyl-1H-1,2,4-triazol-3-yl]-N-(2,2-difluoroethyl)- | [Molecular Formula]
C22H21F2N7O | [MOL File]
2365193-22-0.mol | [Molecular Weight]
437.45 |
| Chemical Properties | Back Directory | [density ]
1.53±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml
Ethanol: Slightly Soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
12.21±0.46(Predicted) | [color ]
Light yellow to light brown |
| Hazard Information | Back Directory | [Uses]
Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma[1][2][3][4]. | [in vivo]
Zelasudil (5-100 mg/kg, p.o., a single dose for 21 days) reduces fibrosis and collagen deposition, suppresses the expression of a number of genes strongly associated with fibrosis in a murine Bleomycin (HY-108345)-induced lung fibrosis model[4].
| Animal Model: | Bleomycin (HY-108345)-induced lung fibrosis mouse model[4] | | Dosage: | 5-100 mg/kg | | Administration: | p.o., a single dose for 21 days | | Result: | Significantly reduced fibrosis and collagen deposition and picrosirius red in the lung. |
| [References]
[1] Lee E, et al. Selective ROCK2 inhibition for treatment of edema and associated conditions: World Intellectual Property Organization, WO2022169946. 2022-08-11.
[2] WHO Drug Information-World Health Organization (WHO).
[3] Pajic M, et al. Combining zelasudil, a small molecule ROCK2 inhibitor, with chemotherapy or immunotherapy improves response in preclinical models of pancreatic cancer[J]. Cancer Research, 2024, 84(6_Supplement): 720-720.
[4] Gambardella A, et al. Effects of RXC007, a highly potent and selective ROCK2 inhibitor, in ex-vivo and in vivo models of pulmonary fibrosis[C]//European Respiratory Journal. 442 GLOSSOP RD, SHEFFIELD S10 2PX, ENGLAND: EUROPEAN RESPIRATORY SOC JOURNALS LTD, 2022, 60. |
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