Complement C1s-IN-1

SKU: orb1982594

Description

Complement C1s-IN-1 is a potent, selective, and orally bioavailable C1s inhibitor that blocks the classical pathway. Its brain-penetrant properties make it a valuable tool for researching complement-driven pathologies in neurological disorders, as evidenced by its dose-dependent inhibition of MAC formation in human serum and its use in relevant in vivo models.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 3033831-40-9
• MW: 422.43
• Purity: 97.77% (May vary between batches)
• Formula: C₂₂H₂₀F₂N₆O
• SMILES: CC1=CC([C@@H]2N(CCN(C2)C3=CC4=C(C(F)=C3)C(N)=NN=C4)C5=CC(F)=CC=C5)=NO1
• Target: Complement System

Bioactivity

• Target IC50:
  C1s (human):36 nM|Other serine proteases:>30,000 nM|C1s (mouse):61 nM
• In Vivo:
  Following oral administration in mice (10–100 mg/kg), Complement C1s-IN-1 showed dose-dependent plasma exposure (Cmax up to 8895.5 ng/mL; AUC₀–₂₄h = 139,341 ng·h/mL) with a mean residence time of 7.66 h. Complement C1s-IN-1 exhibited strong brain penetration, with brain concentrations reaching 33,559.5 ng/g at 2 h and a brain/plasma ratio up to 1.7.
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• In Vitro:
  Complement C1s-IN-1 (compound (R)-8) is a highly selective C1s inhibitor with an IC₅₀ of 36 nM for human C1s and 61 nM for mouse C1s. Complement C1s-IN-1 showed minimal activity against other serine proteases (IC₅₀ > 30,000 nM). Complement C1s-IN-1 also dose-dependently inhibited serum-induced classical complement pathway activation in vitro.
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Storage & Handling

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

Compound Identifiers

PubChem CID

171378331