BIM5078

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BIM5078

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Cat No: 12031

Biochemicals - Receptor Pharmacology

HNF4α is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BIM5078 is an HNF4α antagonist that can repress the exp...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

1-[(2-chloro-5-nitrophenyl)sulfonyl]-2-methyl-1H-benzimidazole

Correlated keywords:

HNF4? nuclear receptors transcription factors glucose homeostasis lipids, antagonists insulin promoters genes expressions hepatocytes steatosis apoptosis cancers hepatocellular carcinoma HNF4.alpha. HNF4a HNF4alpha BIM-5078 BIM 5078 BI-6015, BI6015, BI 6065 HVM

Product Overview:
HNF4α is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BIM5078 is an HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in T6PNE cells with an IC50 value of 930 nM.{21357} BIM5078 binds directly to the ligand binding pocket of HNF4α with an EC50 value of 11.9 nM.{21357} However, BIM5078 has unfavorable pharmacokinetic properties including low plasma and microsomal stability (8% remaining after 3 hours and 32% after 1.25 hours, respectively), high binding to plasma proteins (98% bound after 4 hours), and low solubility (0.17 mg/ml after 18 hours).{21357} BI6015 (Item No. 12032) is a structural analog of BIM5078 developed for more favorable pharmacokinetics.

Size	5 mg
Shipping	dry ice
CAS Number	337506-43-1
Molecular Formula	C₁₄H₁₀ClN₃O₄S
SMILES	CC1=NC2=CC=CC=C2N1S(C3=C(Cl)C=CC([N+]([O-])=O)=C3)(=O)=O
Molecular Weight	351,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.