-
Antiviral API
- Arenavirus
- Cytomegalovirus (CMV)
- Endogenous Metabolite
- Enterovirus (EV)
- Epstein-Barr virus (EBV)
- Filovirus
- HCV Protease
- Hepatitis B Virus (HBV)
- Hepatitis C Virus (HCV)
- Herpes simplex Virus (HSV)
- HIF/HIF Prolyl-Hydroxylase
- HIV Integrase
- HIV Protease
- Human immunodeficiency Virus (HIV)
- Human papillomavirus (HPV)
- Influenza Virus
- Orthopoxvirus
- Others
- Respiratory syncytial Virus (RSV)
- Reverse Transcriptases (RTs)
- SARS-CoV
- Virus Protease
- Antiviral intermediates
Tenofovir exalidex
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| Category | Hepatitis B Virus (HBV) |
| CAS | 911208-73-6 |
| Description | Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a highly potent prodrug of the antiviral tenofovir, appeared safe and well-tolerated in patients with hepatitis B, according to a presentation at The Liver Meeting 2017. Tenofovir exalidex results in decreased circulating levels, lowering systemic exposure and thereby reducing the potential for renal and bone side effects. |
Product Information
| Synonyms | 3-(hexadecyloxy)propyl hydrogen ((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate; Tenofovir exalidex; HDP-Tenofovir; Tenofovir; CMX-157; CMX157; CMX 157 |
| IUPAC Name | [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-(3-hexadecoxypropoxy)phosphinic acid |
| Molecular Weight | 569.72 |
| Molecular Formula | C28H52N5O5P |
| Canonical SMILES | C[C@@H](OCP(O)(OCCCOCCCCCCCCCCCCCCCC)=O)CN1C=NC2=C(N)N=CN=C12 |
| InChI | 1S/C28H52N5O5P/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-18-36-19-17-20-38-39(34,35)24-37-25(2)21-33-23-32-26-27(29)30-22-31-28(26)33/h22-23,25H,3-21,24H2,1-2H3,(H,34,35)(H2,29,30,31)/t25-/m1/s1 |
| InChIKey | BPPMYUZIZUESBY-MLEONAHRSA-N |
| Boiling Point | 706.9±70.0 °C at 760 Torr |
| Purity | ≥98% (HPLC) |
| Density | 1.18±0.1 g/cm3 |
| Solubility | Soluble in DMSO |
| Appearance | White to off-white solid powder |
| Application | Anti-HIV Agents |
| Storage | Store in a cool and dry place (or refer to the Certificate of Analysis). |
| Complexity | 650 |
| Exact Mass | 569.37060677 |
| In Vitro | Tenofovir exalidex is consistently >300-fold more active than Tenofovir against multiple viruses in several different cell systems. Tenofovir exalidex will be effective against MNR mutants, including those that are unresponsive to all currently available NRTIs. Notably, the average EC50 in PBMCs for CMX157 against a panel of 27 wild-type HIV-1 isolates representing group M subtypes A to G and group O was 2.6 nM (range, 0.2 to 7.2 nM). Tenofovir exalidex exerts its therapeutic actions by inhibiting HBV polymerase-mediated HBV DNA elongation, but there is no known binding of cyclophilins to HBV polymerase nor participation of cyclophilins in DNA elongation. The combinational effect of CRV431 (host-targeting) and Tenofovir exalidex (direct-acting) on HBV DNA production is more consistent with the two compounds acting on distinct steps of the HBV life cycle. |
| In Vivo | Tenofovir exalidex (Sprague-Dawley rats) is orally available and has no apparent toxicity when given orally to rats for 7 days at doses of 10, 30, or 100 mg/kg/day.Tenofovir exalidex (5-10 mg/kg; oral gavage; daily for a period of 16 days) decreases liver HBV DNA levels dose-dependently. Animal Model: Female transgenic mice HBV transgenic Tg05 mice (C57BL/6) Dosage: 5 mg/kg, 10 mg/kg Administration: Oral gavage; daily for a period of 16 days Result: The reductions in HBV DNA were 55% and 97% for low-dose (5 mg/kg/day) and high-dose (10 mg/kg/day), respectively. |
| PSA | 144.42000 |
| Target | HIV; HBV; Nucleoside Antimetabolite/Analog |
| XLogP3-AA | 6.7 |
