NOSO-502

NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties^[1]. In Vitro:NOSO-502 (16 µg/mL and 32 µg/mL; 24 h) causes E.coli ATCC 25922 and K. pneumoniae ATCC 43816 strains develop resistance to NOSO-502^[1].
NOSO-502 (100 µM) decreases the activity of HRPTEpiC cells, but insignificantly increases the expression of heat shock protein 27 (HSP27) and kidney injury molecule 1 (KIM-1)^[1].
Antibacterial in vitro activities of NOSO-502^[1]

	Citrobacter freundii DSM 30039	Citrobacter kozeri DSM 4595	Enterobacter aerogenes DSM 30053	Enterobacter cloacae DSM 14563	Escherichia coli ATCC 25922
MIC (µg/mL)	2	2	2	2	4

	Klebsiella pneumoniae ATCC 43816	Serratia marcescens DSM 17174	Stenotrophomonas maltophilia ATCC 13637	Staphylococcus aureus ATCC 29213	Staphylococcus epidermidis ATCC 12228
MIC (µg/mL)	1	4	16	1	0.25

In Vivo:NOSO-502 (1.3-40 mg/kg; s.c.; single dose) shows antibacterial activity in NMRI mice infected E. coli EN122^[1].
NOSO-502 (4-24 mg/kg; s.c.; single dose) shows protective effect in C3H/HeN mice infected E. coli UTI89^[1].
NOSO-502 (2-80 mg/kg; s.c.; single dose) shows protective effect in CD-1/ICR mice infected K. pneumoniae NCTC 13442^[1].
Pharmacokinetic (PK) parameters of NOSO-502^[1]

Species	Route	Dose (mg/kg)	Cmax (mg/L)	AUC0-Tlast (mg/L•h)	Vd (L/kg)	T1/2 (min)	Clearance (L/h/kg)
Mouse	Intravenous injection	30	23.46	8.88	0.66	25	1.13
Rat	Intravenous injection	15	40.70	7.99	0.94	90	1.92