NOSO-502 is a bacterial translation inhibitor. NOSO-502 has inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties.

Physicochemical Properties

Molecular Formula	C47H80FN17O11
Molecular Weight	1078.24381256104
CAS #	1894081-09-4
PubChem CID	134817194
Appearance	Typically exists as solid at room temperature
Hydrogen Bond Donor Count	17
Hydrogen Bond Acceptor Count	19
Rotatable Bond Count	36
Heavy Atom Count	76
Complexity	1970
Defined Atom Stereocenter Count	8
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	NOSO-502 imparts resistance to NOSO-502 in E (16 µg/mL and 32 µg/mL; 24 h). K. coli and ATCC 25922. strains of pneumoniae ATCC 43816 [1]. The HRPTEpiC cell viability was decreased by NOSO-502 (100 µM), while the expression of kidney injury molecule 1 (KIM-1) and heat shock protein 27 (HSP27) was not significantly increased [1]. The in vitro antibacterial activity of NOSO-502 has been reported [1] against Citrobacter freundii DSM 30039, Citrobacter kozeri DSM 4595, Enterobacter aerogenes DSM 30053, Enterobacter cloacae DSM 14563, and Escherichia coli ATCC 25922 MIC (µg/mL) 2 2 2 2 4 Klebsiella pneumoniae ATCC 4381 6 Serratia marcescens DSM 17174, Stenotrophomonas maltophilia ATCC 13637, Staphylococcus aureus ATCC 29213, and Staphylococcus epidermidis ATCC 12228. MIC (µg/mL) 1 4 16 1 0.25.
ln Vivo	In NMRI mice infected with E. coli, NOSO-502 (1.3–40 mg/kg; subcutaneous injection; single dosage) has antibacterial activity. Coli EN122 [1]. In C3H/HeN mice infected with E, NOSO-502 (4-24 mg/kg; subcutaneous injection; single dosage) has protective effects. Coli UTI89 [1]. The subcutaneous injection of NOSO-502 (2-80 mg/kg; single dosage) provides protection against Klebsiella pneumoniae NCTC 13442 infection in CD-11/ICR mice [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 are the pharmacokinetic (PK) properties of NOSO-502 [1].
Animal Protocol	Animal/Disease Models: Female NMRI mice infected E. coli EN122[1]. Doses: 1.3, 2.5, 5, 10, 20, and 40 mg/kg. Route of Administration: subcutaneous (sc)injection; single dose. Experimental Results: demonstrated anti-infective effect. Animal/Disease Models: Female C3H/HeN mice infected E. coli UTI89[1]. Doses: 4, 12 and 24 mg/kg. Route of Administration: subcutaneous (sc)injection; single dose. Experimental Results: Dramatically attenuated E. coli UTI89 damage to urine, bladder, kidneys, and improved survival rates. Animal/Disease Models: Male CD-1/ICR mice infected K. pneumoniae NCTC 13442[1]. Doses: 2, 6, 20 and 80 mg/kg. Route of Administration: subcutaneous (sc)injection; single dose. Experimental Results: Dramatically improved lung tissue damage.
References	[1]. Racine E, et al. In Vitro and In Vivo Characterization of NOSO-502, a Novel Inhibitor of Bacterial Translation. Antimicrob Agents Chemother. 2018 Aug 27;62(9):e01016-18.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.9274 mL	4.6372 mL	9.2744 mL
	5 mM	0.1855 mL	0.9274 mL	1.8549 mL
	10 mM	0.0927 mL	0.4637 mL	0.9274 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.