WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H327026
CAS#: 911208-73-6
Description: Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a novel lipid acyclic nucleoside phosphonate that delivers high intracellular concentrations of the active antiviral agent tenofovir. Tenofovir exalidex results in decreased circulating levels, lowering systemic exposure and thereby reducing the potential for renal and bone side effects. Potential Advantages of Tenofovir exalidex over Tenofovir include: Increased efficacy by boosting bioavailability; Takes advantage of natural lipid uptake mechanisms; Decreased renal toxicity by reduced circulating TFV; 97-fold more active against HBV in vitro.
Hodoodo Cat#: H327026
Name: Tenofovir exalidex
CAS#: 911208-73-6
Chemical Formula: C28H52N5O5P
Exact Mass: 569.37
Molecular Weight: 569.730
Elemental Analysis: C, 59.03; H, 9.20; N, 12.29; O, 14.04; P, 5.44
Synonym: Tenofovir exalidex; HDP-Tenofovir; Tenofovir; CMX-157; CMX157; CMX 157
IUPAC/Chemical Name: 3-(hexadecyloxy)propyl hydrogen ((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate
InChi Key: BPPMYUZIZUESBY-MLEONAHRSA-N
InChi Code: 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
SMILES Code: C[C@@H](OCP(O)(OCCCOCCCCCCCCCCCCCCCC)=O)CN1C=NC2=C(N)N=CN=C12
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 569.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Lanier ER, Ptak RG, Lampert BM, Keilholz L, Hartman T, Buckheit RW Jr, Mankowski MK, Osterling MC, Almond MR, Painter GR. Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. Antimicrob Agents Chemother. 2010 Jul;54(7):2901-9. doi: 10.1128/AAC.00068-10. Epub 2010 May 3. PubMed PMID: 20439609; PubMed Central PMCID: PMC2897300.
2: Hostetler KY. Alkoxyalkyl prodrugs of acyclic nucleoside phosphonates enhance oral antiviral activity and reduce toxicity: current state of the art. Antiviral Res. 2009 May;82(2):A84-98. PubMed PMID: 19425198; PubMed Central PMCID: PMC2768545.
3: Quenelle DC, Collins DJ, Pettway LR, Hartline CB, Beadle JR, Wan WB, Hostetler KY, Kern ER. Effect of oral treatment with (S)-HPMPA, HDP-(S)-HPMPA or ODE-(S)-HPMPA on replication of murine cytomegalovirus (MCMV) or human cytomegalovirus (HCMV) in animal models. Antiviral Res. 2008 Aug;79(2):133-5. doi: 10.1016/j.antiviral.2008.01.155. Epub 2008 Feb 22. PubMed PMID: 18336926; PubMed Central PMCID: PMC2650230.
4: Painter GR, Almond MR, Trost LC, Lampert BM, Neyts J, De Clercq E, Korba BE, Aldern KA, Beadle JR, Hostetler KY. Evaluation of hexadecyloxypropyl-9-R-[2-(Phosphonomethoxy)propyl]- adenine, CMX157, as a potential treatment for human immunodeficiency virus type 1 and hepatitis B virus infections. Antimicrob Agents Chemother. 2007 Oct;51(10):3505-9. Epub 2007 Jul 23. Erratum in: Antimicrob Agents Chemother. 2007 Dec;51(12):4538. PubMed PMID: 17646420; PubMed Central PMCID: PMC2043283.