191425-55-5

Upstream product

• 5070-13-3 bis-(p-nitrophenyl) carbonate 
• 15100-75-1 L-phenylalanine tert-butyl ester hydrochloride 
• 16874-17-2 L-phenylalanine tert-butyl ester 
• 7693-46-1 4-Nitrophenyl chloroformate 

Downstream Products

• 1138406-13-9 4'-O-(CO-Phe-OtBu)-quercetin 
• 1138406-41-3 3′-O-CO-(Phe-OtBu)quercetin 
• 1138406-20-8 4'-O-(CO-Phe-OH)-quercetin 
• 1138406-28-6 3'-O-(CO-Phe-OH)-quercetin 
• 1270004-51-7 4'-O-CO-(Phe-OtBu)-tricin 

Relevant academic research and scientific papers

Traversal of the Blood-Brain Barrier by Cleavable l -Lysine Conjugates of Apigenin

Apigenin, a flavone abundant in parsley and celery, is known to act on several CNS receptors, but its very poor water solubility (a temporary sedative effect on the mice within 5 min of intraperitoneal administration (single dose of 0.4 mg/g) and could be detected in the mice brain tissues at a concentration of 0.82 μg/g of intact Lys-apigenin carbamate 10 and 0.42 ug/g of apigenin at 1.5 h. This study accomplished the delivery of apigenin across the BBB in a manner that might be applicable to other congeners, which should inform the future development of BBB-crossing flavonoids.

Synthesis and biochemical evaluation of baicalein prodrugs

Baicalein (5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one), a flavonoid analog from Scutellaria baicalensis, possesses several pharmacological activities including antioxidant, antiprolif-erative, and anti-inflammatory activities. We previously reported

CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS

The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.

1,2,4-Oxadiazole Compounds as Inhibitors of CD47 Signalling

The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the tre

Heterocyclic derivatives with immunomodulatory effects

The invention relates to novel heterocyclic derivatives with immunomodulatory effects capable of inhibiting therapeutic agents in a programmed cell death (PD1) signal path. The compounds disclosed bythe invention are capable of enhancing antitumor activit

Increased bioavailability of tricin-amino acid derivatives via a prodrug approach

Tricin (4′,5,7-trihydroxy-3′,5′-dimethoxyflavone) has demonstrated diverse biological activities. This compound has a high anti-human cytomegalovirus (HCMV) activity; however, its oral availability is low. To improve its bioavailability, we synthesized tricin-amino acid derivatives as prodrugs and investigated their cell permeability, stability in vitro, and oral availability in vivo. The results demonstrated that the tricin-alanine-glutamic acid conjugate exhibited enhanced permeability, stability in MDCK cells, and excellent bioavailability after oral administration in Crl:CD (SD) male rats. Tricin-alanine-glutamic acid conjugate is a potential new anti-HCMV drug.

In vitro solubility, stability and permeability of novel quercetin-amino acid conjugates

In order to discover a quercetin prodrug with improved bioavailability, we synthesized nine quercetin-amion acid conjugates and estimated their pharmacokinetic properties including water solubility, stability against chemical or enzymatic hydrolysis, and