Lefamulin(BC-3781)|novel antibiotic

Cas No.:	1350636-82-6
Chemical Name:	(3aS,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propano-3aH-cyclopenta[8]annulen-8-yl {[(1R,2R,4R)-4-amino-2-hydroxycyclohexyl]sulfanyl}acetate
Synonyms:	BC-3781,BC 3781,BC3781
SMILES:	O=C(O[C@H]1[C@@]([C@H](C)CC2)(C)[C@@](C(CC3)=O)([H])[C@]32[C@@H](C)[C@H](O)[C@](C)(C=C)C1)CS[C@H]4[C@H](OC(C)=O)C[C@H](N)CC4
Formula:	C₃₀H₄₇NO₆S
M.Wt:	549.76
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment. Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer[1].
In Vitro:	Lefamulin acetate (BC-3781 acetate) has activity against the resistant gram-postive organisms, including taphylococcus aureus (MRSA) (MIC50=0.12 μg/ml; MIC90=0.25 μg/ml); β-Hemolytic strepococcus (MIC50=0.03 μg/ml; MIC90=0.03 μg/ml); Viridans group Streptococcus (MIC50=0.12 μg/ml; MIC90=0.5 μg/ml), Enterocossus faecium (MIC50=0.12 μg/ml; MIC90=4 μg/ml), Streptococcus pneumonia (MIC50=0.12 μg/ml; MIC90=0.25 μg/ml)[1]. Lefamulin has activity against gram-negative organisms, including Haemophilus influenza (MIC50=1 μg/ml; MIC90=0.12 μg/ml) and Moraxella cotarrhali (MIC50=2 μg/ml; MIC90=0.25 μg/ml)[1].
References:	[1]. Veve MP, et al. Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic. Pharmacotherapy. 2018 Sep;38(9):935-946. doi: 10.1002/phar.2166. Epub 2018 Aug 20.

Cat. No.	Product name	Field of application
DC75721	CL2A-SN38 (Govitecan)	CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .
DC47877	tri-GalNAc-COOH (acetylation)	tri-GalNAc-COOH acetylation is the acetylated and modified form of tri-GalNAc-COOH. tri-GalNAc-COOH acetylation can be used for the synthesis of LYTAC.
DC46965	Tri-GalNAc-COOH	tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.
DC46471	RP101988	RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
DC37901	PD-173212	PD-173212 is a small molecule N-type calcium channel blocker.
DC37333	N,N-Diethyl-p-toluamide	N,N-Diethyl-p-toluamide is a mosquito repellent.
DC37321	AI3-15902	AI3-15902 is a biochemical.
DC37283	Methyl phenylcarbamate	Methyl phenylcarbamate is a biochemical.
DC37252	Ampyrone	Ampyrone is a metabolite of AMINOPYRINE with analgesic and anti-inflammatory properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. Ampyrone stimulates LIVER MICROSOMES and is also used to measure extracellular water.
DC37245	Piperonyl butoxide	Piperonyl butoxide (PBO) is an organic compound used as a component of pesticide formulations. It is a waxy white solid. It is a synergist. That is, despite having no pesticidal activity of its own, it enhances the potency of certain pesticides such as carbamates, pyrethrins, pyrethroids, and rotenone.[1] It is a semisynthetic derivative of safrole.

Lefamulin acetate