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CA-074 methyl ester

SKU: orb1223286

Description

Ca-074Me is a selective and cell-permeable inhibitor of cathepsin B.(In Vitro):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.. CA-074Me reduces apoptosis induced by CVB1.\n(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. CA-074Me (30 mg/kg) is capable of inhibiting osteoclastogenesis and bone degradation in vivo. 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.

Images & Validation

Key Properties

CAS Number147859-80-1
MW397.5
Purity>98% (HPLC)
FormulaC19H31N3O6
SMILESCCCNC(=O)[C@@H]1[C@H](O1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1CCC[C@@H]1C(=O)OC
TargetPKC
SolubilityDMSO : ≥ 215 mg/mL. 540.92 mM; H2O : 26.66 mg/mL. 67.07 mM;

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

LY300046

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  • CA-074 methyl ester [orb1304217]

    97.26% (May vary between batches)

    147859-80-1

    397.47

    C19H31N3O6

    2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO)
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Protocol Information

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