Bio.etc Pte Ltd | [MCE]: NEW SMALL MOLECULES FOR MAY 2021

17 May [MCE]: NEW SMALL MOLECULES FOR MAY 2021

Posted at 03:45h in News by Editorial Bio.etc

0 Likes

MCE (MedChemExpress) provides a wide range of lifescience biochemicals, including more than 25,000 bioactive compounds, dye reagents, peptides and natural compounds for laboratory and scientific use.

JMV 449 acetate
Research Area: GPCR/Neurotensin Receptor/Neurological Disease

• Potent neurotensin receptor agonist (IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum).
• Highly potent and long-lasting hypothermic and analgesic effects in the mouse. Solubility: H2O : 100 mg/mL (123.91 mM; Need ultrasonic)

CAS No.: 344900-92-1
FTI-2153
Research Area: Metabolic Enzyme/Farnesyl Transferase/Lung Cancer

• Potent and highly selective farnesyltransferase (FTase) inhibitor (IC50=1.4 nM).
• >3000-fold more potent at blocking H-Ras (IC₅₀, 10 nM) than Rap1A processing.
• Blocks bipolar spindle formation and chromosome alignment.

Solubility: DMSO : 100 mg/mL (214.32 mM; Need ultrasonic)

CAS No.: 142715-48-8
CP-100356 hydrochloride
Research Area: Membrane Transporter/Ion Channel/Drug Metabolite

• Potent, orally active dual MDR1 (P-gp)/BCRP inhibitor.
• Inhibits MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport (IC₅₀=0.5 and 1.5 µM, respectively).

Solubility: DMSO : 44 mg/mL (73.69 mM; Need ultrasonic and warming)

CAS No.: 2068119-11-7
S18-000003
Research Area: Lipid Metabolism/ROR/Psoriasis

• Potent, selective and orally active inhibitor of RORγt (IC₅₀ of
• Inhibits Th17 cell differentiation from human naive CD4+ T cells with an IC₅₀ of 24 nM.
• For the research of psoriasis with low risk of thymic aberrations.

Solubility: DMSO : 100 mg/mL (192.85 mM; Need ultrasonic)

CAS No.: 909561-15-5
AS1810722
Research Area: JAK/STAT Signaling/Asthma/Atopic Diseases

• Potent and orally active STAT6 inhibitor (IC₅₀=1.9 nM) and shows a good CYP3A4 inhibition profile.
• Inhibits in vitro Th2 differentiation (IC50=2.4 nM) and inhibits production of IL-4 (IC₅₀=2.4 nM).
• Suppresses eosinophil infiltration in an antigen-induced mouse asthmatic model.

Solubility: DMSO : 62.5 mg/mL (130.89 mM; Need ultrasonic)

CAS No.: 1075240-43-5
Omadacycline tosylate
Research Area: Gram-negative/Gram-positive Bacterial Infection

• First-in-class orally active aminomethylcycline antibacterial.
• Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit.
• Possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria.

Solubility: H₂O : 12.5 mg/mL (17.15 mM; Need ultrasonic

JC-1 Mitochondrial Membrane Potential Assay Kit

MCE JC-1 Mitochondrial Membrane Potential Assay Kit consists of JC-1, Phosphate-buffered saline (10×) and CCCP (50 mM in DMSO). The kit uses JC-1 to detect the mitochondrial membrane potential in variety of cell types, as well as intact tissues and isolated mitochondria.

Fragment Library

Fragment-based drug discovery (FBDD) has become an attractive strategy to develop hits in target-based drug discovery. Several drugs derived from fragment-based approach have been approved by FDA and avariety of drugs have entered clinical studies. MCE fragment library, containing 14,000+ fragment compounds, is an important source of lead-like drugs.