- PRODUCT NAME:Apabetalone
1.What is Apabetalone?
Apabetalone is a highly effective BET bromodomain inhibitor that specifically targets the BD2 domain.
2.How it Works?
Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor that selectively targets BD2, with an IC50 of 0.510 μM in cell-free assays, showing 170-fold selectivity over BD1.
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RVX-208 is a potent bromodomain inhibitor targeting both BD2 and BD1, with IC50 values of 0.51 μM and 87 μM, respectively.
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Bromodomains (BRDs) are protein interaction modules that bind to proteins containing ε-N-acetyllysine. BRDs act as effector domains for chromatin-modifying enzymes, transcriptional regulators, and chromatin regulators.
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RVX-208 is a potent inhibitor of Class II BET bromodomains. It exhibits affinity for both BD2 and BD1, with KD values of 0.194 μM and 4.06 μM, respectively. RVX-208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner[1].
Mechanism of Action
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In HepG2 cells, RVX-208 induces the messenger RNA and protein synthesis of apolipoprotein (apo) A-I. It also induces BRD4-mediated ApoA-I mRNA expression.
In Vivo Effects
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In African green monkeys, RVX-208 increases serum HDL-C and apoA-I levels by 97% and 60%, respectively.
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RVX-208 also increases pre-β1-LpA-I, α1-LpA-I HDL subparticles, ATP-binding cassette transporter G1 (ABCG1), ATP-binding cassette transporter A1 (ABCA1), and cholesterol efflux.
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In hyperlipidemic apoE(-/-) mice, RVX-208 (150 mg/kg) significantly inhibits aortic lesion formation. Additionally, it increases HDL-C, reduces LDL-C, and decreases pro-inflammatory cytokines.
3.Benefits and Uses：
Apabetalone is being investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.
4.Q&A
Q:Does the company accept sample orders?
A:Yes, our company accepts sample orders.
Q:What is the minimum order quantity for the company?
A:We do not have a minimum order quantity requirement, we arrange according to the customer's needs.
Q:How to ensure the quality of goods?
A:We have a strict QC/QA management system and strict release procedures, and we will provide all procedures to customers before shipment according to their requirements.
Q:Can we see the product quality before the order is shipped?
A:Of course, we always provide a relative Batach (s) 'COA before shipping.
Q:How will you deliver the goods?
A:We will communicate with customers, adopt their suggestions, arrange the most suitable delivery method, and ensure mutual satisfaction.
