| Bioactivity | CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects. | |||||||||
| Invitro | CA-074Me (5 μM and 50 μM) inhibits RANKL-induced osteoclastogenesis in BMM cells derived from C57BL/6J and NOD/ShiLtJ mice. CA-074Me exerts its anti-osteoclastogenic effect within 24 hours post-RANKL stimulation in vitro. CA-074Me does not exert its anti-osteoclastogenic effect via the MAPK-ERK signaling cascade. CA-074Me inhibits c-FOS upregulation and subsequent NFATc1 autoamplification following RANKL stimulation.[2]. CA-074Me reduces apoptosis induced by CVB1[3]. | |||||||||
| In Vivo | Hippocampal CA1 neuronal programmed necrosis induced by global cerebral I/R injury is prevented by CA074-me (1 μg, 10 μg) both pre-treatment and post-treatment. The rupture of lysosomal membrane and the leakage of cathepsin-B, and this is strongly inhibited by CA074-me pre-treatment. The overexpression and nuclear translocation of RIP3 and the reduction of NAD+ level after I/R injury are also inhibited, while the upregulation of Hsp70 is strengthened by CA074-me pre-treatment[1]. CA-074Me (30 mg/kg) is capable of inhibiting osteoclastogenesis and bone degradation in vivo[2]. In the CVB+CA-074Me (4 mg/kg/day i.m.) guinea pigs group, the scores of inflammation significantly decrease in comparison with the CVB+None group. In CVB+CA-074Me group, the number of CD8+T cells decrease in comparison with the sham group[3]. | |||||||||
| Name | CA-074 methyl ester | |||||||||
| CAS | 147859-80-1 | |||||||||
| Formula | C19H31N3O6 | |||||||||
| Molar Mass | 397.47 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Xu Y, et al. Protective mechanisms of CA074-me (other than cathepsin-B inhibition) against programmed necrosis induced by global cerebral ischemia/reperfusion injury in rats. Brain Res Bull. 2016 Jan;120:97-105 [2]. Patel N, et al. CA-074Me compound inhibits osteoclastogenesis via suppression of the NFATc1 and c-FOS signaling pathways. J Orthop Res. 2015 Oct;33(10):1474-86 [3]. Zhang L, et al. Treatment with CA-074Me, a Cathepsin B inhibitor, reduces lung interstitial inflammation and fibrosis in a rat model of polymyositis. Lab Invest. 2015 Jan;95(1):65-77 |
CA-074 methyl ester
CAS: 147859-80-1 F: C19H31N3O6 W: 397.47
CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti
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