CA-074 methyl ester

CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

Product information

CAS Number: 147859-80-1

Molecular Weight: 397.47

Formula: C19H31N3O6

Chemical Name: methyl 1-(3-methyl-2-{[3-(propylcarbamoyl)oxiran-2-yl]formamido}pentanoyl)pyrrolidine-2-carboxylate

Smiles: CC(CC)C(NC(=O)C1OC1C(=O)NCCC)C(=O)N1CCCC1C(=O)OC

InChiKey: XGWSRLSPWIEMLQ-UHFFFAOYSA-N

InChi: InChI=1S/C19H31N3O6/c1-5-9-20-16(23)14-15(28-14)17(24)21-13(11(3)6-2)18(25)22-10-7-8-12(22)19(26)27-4/h11-15H,5-10H2,1-4H3,(H,20,23)(H,21,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (251.59 mM; Need ultrasonic). H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.