Tenofovir exalidex

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.

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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