InterBioTech FT-XLS250 Entecavir Product Description Catalog #: XLS250, 5mg XLS251, 10mg XLS252, 50mg XLS253, 100mg AXAIV0, 1ml 10mM in DMSO. Catalog #: Name: Entecavir, Monohydrate Syn: BMS200475 monohydrate; SQ34676 monohydrate CAS : 209216-23-9 MW : 295.29 Formula : C12H17N5O4 Properties : DMSO : ≥ 50 mg/mL (169.33 mM) H2O : 2.8 mg/mL (9.48 mM) >99.5% Storage: Powder: -20°C (long term; possible at +4°C (2 years) (M) Also available: In solvent: -80°C (6 months) -20°C (1 month) Entecavir free form #RO893P/Q/R (Syn.: BMS200475; SQ34676) CAS No. : 142217-69-4; MW: 277.2 For Research Use Only Introduction Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell. IC50 & Target EC50：3.75 nM (anti-HBV, HepG2 cell)[1] In Vitro *Solubility : DMSO : ≥ 50 mg/mL (169.33 mM) H2O : 2.8 mg/mL (9.48 mM; Need ultrasonic and warming) *Preparation : 1mM = 1mg in 3.3865 mL Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) has a EC50 of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses[1]. Entecavir monohydrate is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2]. P.1 InterBioTech FT-XLS250 In Vivo *Preparation : 1. Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution 2. Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution 3. Add each solvent one by one: 10% DMSO 90% corn oil Solubility: ≥ 3 mg/mL (10.16 mM); Clear solution Daily oral treatment with Entecavir monohydrate at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks[3]. References [1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(1 1):1845-56. [3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. More: •Mol Pharm. 2018 Oct 30. •Virus Res. 2019 Jul 31:197677. Related products Related Small Molecules: antiviral compounds Vesatolimod #WPY994 (CAS :1228585-88-3 ; MW : 410.5) Bay 41-4109 (Bayer 41-4109) #AX5V71 (CAS :298708-81-3; MW:395.76) 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) #1M8596 (CAS : 57378-72-0 ; MW :516.4) Morphothiadin (GLS4) #AYHNG1 (CAS : 1092970-12-1 ; MW : 509.39) AB-423 #B2VBA1 (CAS : 1572510-80-5 ; MW ; 386.39) Squalamine (MSI-1256) #PM9151 (CAS : 148717-90-2 ; MW : 627.96) Ordering information Catalog size quantities and prices may be found at http://www.interchim.com. Please inquire for higher quantities (availability, shipment conditions). Please contact InterBioTech – Interchim for any other information Hotline : +33(0)4 70 03 73 06 – [email protected] Disclaimer : Materials are sold for research use only, and are not intended for food, drug, household, or cosmetic use. Interchim ® is not liable for any damage resulting from handling or contact with this product. S01E P.2 .