LB244

• CAT Number: I040719
• Molecular Formula: C30H27N5O5
• Molecular Weight: 537.57
• Purity: ≥95%
• Synonyms: N-[(5S)-5-(1H-benzimidazol-2-yl)-5-[(4-phenylbenzoyl)amino]pentyl]-5-nitrofuran-2-carboxamide
• InChI: InChI=1S/C30H27N5O5/c36-29(22-15-13-21(14-16-22)20-8-2-1-3-9-20)34-25(28-32-23-10-4-5-11-24(23)33-28)12-6-7-19-31-30(37)26-17-18-27(40-26)35(38)39/h1-5,8-11,13-18,25H,6-7,12,19H2,(H,31,37)(H,32,33)(H,34,36)/t25-/m0/s1
• InChIKey: YJTWDEBBCCREDG-VWLOTQADSA-N
• SMILES: C1=CC=C(C=C1)C2=CC=C(C=C2)C(=O)NC(CCCCNC(=O)C3=CC=C(O3)[N+](=O)[O-])C4=NC5=CC=CC=C5N4

LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC50=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice[1].
Pharmacokinetic results of LB244 (10 mg/kg, po; 5 mg/kg, ip) in mice showed limited oral activity (Cmax=0.04 μM) and short half-life ( T1/2=2.8 h). Its body clearance is 2854.3 mL/min/kg[1].

Reference

[1]. Barasa L, et al. Development of LB244, an Irreversible STING Antagonist. J Am Chem Soc. 2023 Sep 20;145(37):20273-20288..
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