High Purity 99% BMS-262084 China Supplier CAS 253174-92-4 For Treating Asthma

Place of Origin China
Brand Name XRD
Certification GMP
Model Number 253174-92-4
Minimum Order Quantity negotiable
Price Inquiry for Negotiable
Packaging Details 1-2 kg / aluminum foil bag, 25kg/ drum, as required
Delivery Time 1-2days after payment received
Payment Terms T/T bank, Western Union, Bitcoin, Etc
Supply Ability 1000KG/ Month

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Product Details
CAS 253174-92-4 Product Name BMS-262084
Type Intermediates Appearance Yellow Powder
Usage For Treating Asthma Alias BMS-262084
Assay 99% Key Words BMS-262084
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99% BMS-262084 Manufacturer CAS 253174-92-4 For Treating Asthma


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Produce name : BMS-262084

CAS number : 253174-92-4

Synonyms: BMS-262084; BMS 262084; BMS262084; CHEMBL71037; UNII-I0IR71971G; I0IR71971G; BDBM50120368; DNC004491.;2-Azetidinecarboxylic acid, 3-(3-((aminoiminomethyl)amino)propyl)-1-((4-(((1,1-dimethylethyl)amino)carbonyl)-1-piperazinyl)carbonyl)-4-oxo-, (2S,3R)

BMS‐262084 is a potent and selective β‐lactam tryptase inhibitor with therapeutic potential for treating asthma. The oral bioavailability of BMS‐262084 was low in rats (4% at a dose of 0.5 mg/kg) due to poor absorption. BMS‐262084 was excreted mainly unchanged in the urine, suggesting minimal metabolism in rats. The objective of this study was to investigate the mechanisms of oral absorption of BMS‐262084 in rats. Modulation of intestinal tight junctions, binding to trypsin, and involvement of the intestinal dipeptide transport system and P‐glycoprotein (P‐gp) in the absorption of BMS‐262084 were examined. Coadministration of BMS‐262084 with SQ‐29852, a substrate of the intestinal dipeptide transport system, did not change the oral absorption of BMS‐262084. An increase in the dose of BMS‐262084 from 0.5 to 50 mg/kg resulted in a 3.7‐fold increase in its oral absorption. Inulin absorption was enhanced upon coadministration with BMS‐262084, suggesting the opening of tight junctions in the intestinal epithelium. Coadministration of aprotinin, a trypsin inhibitor, increased the oral absorption of BMS‐262084 several fold. In vitro, using Caco‐2 cells, BMS‐262084 appeared to be a P‐gp substrate, with an efflux ratio of 14. These results suggest that absorption of BMS‐262084 is mediated by several concurrent mechanisms. At higher doses of BMS‐262084, increased absorption may be primarily due to opening of tight junctions in the intestinal epithelium and consequent absorption via the paracellular pathway, while at lower doses, binding to trypsin may contribute to limiting its absorption. P‐gp efflux may also play a role in influencing the absorption of BMS‐262084. The intestinal dipeptide transporter system does not appear to be involved in the absorption of BMS‐262084.




High Purity 99% BMS-262084 China Supplier CAS 253174-92-4 For Treating Asthma 0


99% BMS-262084 Manufacturer CAS 253174-92-4 For Treating Asthma