| Identification | Back Directory | [Name]
Benzeneacetamide, α-(aminomethyl)-4-(hydroxymethyl)-N-6-isoquinolinyl- | [CAS]
1254032-16-0 | [Synonyms]
AR-13503
Benzeneacetamide, α-(aminomethyl)-4-(hydroxymethyl)-N-6-isoquinolinyl- | [Molecular Formula]
C19H19N3O2 | [MOL File]
1254032-16-0.mol | [Molecular Weight]
321.37 |
| Chemical Properties | Back Directory | [Boiling point ]
649.2±55.0 °C(Predicted) | [density ]
1.310±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.89±0.43(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice[1][2]. | [in vivo]
AR-13503 (1.25 mg/kg; i.p.; once daily for 5 days) in collaboration with Aflibercept (HY-108801), significantly decreases the development of aberrant neovascularization (NV)[1].
| Animal Model: | Oxygen-induced retinopathy (OIR) mice model (C57BL/6; 7-days-old)[1] | | Dosage: | 1.25 mg/kg | | Administration: | Intraperitoneal injection; once daily for 5 days | | Result: | The combination group had a greater (~75%) reduction in NV than Aflibercept alone (~55%). |
| [References]
[1] Ding J, et al. ROCK/PKC inhibitor AR-13503 inhibits angiogenesis and protects the barrier function of retinal pigment epithelium[J]. Investigative Ophthalmology & Visual Science, 2018, 59(9): 205-205.
[2] Carbajal K, et al. AR-13503 Enhances the efficacy of aflibercept in a mouse model of proliferative diabetic retinopathy[J]. Investigative Ophthalmology & Visual Science, 2018, 59(9): 200-200. |
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