ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors Sarecycline Hydrochloride

Sarecycline Hydrochloride

Product NameSarecycline Hydrochloride
CAS1035979-44-2
MFC24H30ClN3O8
MW523.97
EINECS
MOL File1035979-44-2.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMF: 0.25 mg/ml,DMSO: 0.25 mg/ml
form	Solid
color	Light yellow to yellow
InChIKey	APPRLAGZQKOUFL-ZKOKXHCXNA-N
SMILES	O[C@@]12C(C(C(=O)N)=C(O)[C@@H](N(C)C)[C@]1([H])C[C@]1([H])CC3=C(C=CC(O)=C3C(=O)C1=C2O)CN(C)OC)=O.Cl \|&1:1,9,13,16,r\|

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

Sarecycline Hydrochloride is a substituted tetracycline compound used for treatment of bacterial infections and neoplasms.

Biological Activity

Sarecycline Hydrochloride iinhibits bacterial protein synthesis by binding to the 30S subunit of the bacterial ribosome. Specifically, it binds to the A site of the ribosome and blocks the attachment of aminoacyl-tRNA molecules to the ribosome, which is necessary for the addition of new amino acids to the growing polypeptide chain. This ultimately leads to the inhibition of bacterial protein synthesis and reduction in bacteria th at are associated with acne.

in vivo

Sarecycline hydrochloride (0.33-9 mg/kg; i.v.) show potent activity against S. aureus in a murine neutropenic thigh infection model^[1].
Sarecycline can inhibit S. aureus (PD₅₀=0.25 mg/kg), but has no significant effect on E. coli even at the highest dose (>40 mg/kg) in CD-1 mice model of systemic (intraperitoneal) infection^[6].
Sarecycline (1-150mg/kg; Intraperitoneal injection; Single dose) shows anti-inflammatory activity in Sprague Dawley rats model^[6].

Animal Model:	Female SD-1 mice (A murine neutropenic thigh wound infection model)^[1]
Dosage:	0.33, 1, 3, or 9mg/kg
Administration:	Intravenously
Result:	Achieved a 2-log10 reduction in the bacterial burden in the thigh at a dose comparable to that of doxycycline, with ED50s of 8.23 and 8.32mg/kg, respectively.

Animal Model:	Carrageenan-induced footpad edema male Sprague Dawley rats model^[6]
Dosage:	1 mg/kg, 5 mg/kg ,10 mg/kg, 25 mg/kg, 50 mg/kg, 75 mg/kg,100 mg/kg, 150 mg/kg
Administration:	Intraperitoneal injection (i.p.); Single dose. Before a subplantar injection of sterile 1 mg/0.1 mL carrageenan solution in the right hind paw.
Result:	Reduced inflammation to 55.7% and 53.1%, respectively, at doses of 75 mg/kg and 100 mg/kg compared to baseline.

IC 50

Tetracycline

Preparation Products And Raw materials