Cathepsin Inhibitor 1

SKU: orb1301150

Description

Cathepsin Inhibitor 1 is a broad-spectrum small molecule inhibitor that potently targets cathepsins L, L2, S, K, and B with varying pIC50 values. This compound is a valuable research tool for studying protease function in areas such as cancer, bone resorption, and immune response, both in cellular assays and animal models.

Research Area

Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 225120-65-0
• MW: 401.89
• Purity: 99.78% (May vary between batches)
• Formula: C₂₀H₂₄ClN₅O₂
• SMILES: Cn1nc(cc1C(=O)NC(Cc1cccc(Cl)c1)C(=O)NCC#N)C(C)(C)C
• Target: Cysteine Protease
• Solubility: Ethanol:47 mg/mL (116.95 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:74 mg/mL (184.13 mM)

Bioactivity

• Target IC50:
  Cathepsin L:7.9(pIC50)|Cathepsin S:6(pIC50)|Cathepsin B:5.2(pIC50)|Cathepsin L2:6.7(pIC50)|Cathepsin K:5.5(pIC50)
• In Vivo:
  Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CysteineProtease, Cysteine Protease, Cathepsin inhibitor1, Cathepsin inhibitor-1, Cathepsin K, Cathepsin Inhibitor 1, Cathepsin, CatB, Cathepsin L2, Cathepsin L, Cathepsin S, CatL2, CatS, CatK, CatL, Inhibitor, inhibit

Compound Identifiers

PubChem CID

56664471