| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Tenofovir exalidex (formerly known as HDP-Tenofovir and CMX-157) is a novel and potent lipophilic / acyclic nucleoside phosphonate that is able to deliver high concentrations of the active antiviral agent tenofovir to target cells. 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 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.
| Targets |
HIV-1;HIV-2
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|---|---|
| ln Vitro |
Tenofovir exalidex exhibits a consistent >300-fold increase in activity compared to Tenofovir against various viruses across multiple cell systems. Tenofovir exalidex is effective against MNR mutants, including those that don't react to any of the NRTIs that are on the market right now. CMX157's average EC50 in PBMCs was 2.6 nM (range, 0.2 to 7.2 nM) against a panel of 27 wild-type HIV-1 isolates representing group M subtypes A to G and group O. This is noteworthy[1].
Although cyclophilins are not known to bind to HBV polymerase or participate in DNA elongation, tenofovir exalidex works as a therapeutic by blocking HBV polymerase-mediated HBV DNA elongation. Tenofovir exalidex (direct-acting) and CRV431 (host-targeting) together have a combination effect on HBV DNA production that is more consistent with the two drugs acting on different stages of the HBV life cycle[3]. |
| ln Vivo |
Oral administration of tenofovir exalidex (Sprague-Dawley rats) at doses of 10, 30, or 100 mg/kg/day to rats for seven days does not appear to be toxic[2]. Metovir exalidex (5–10 mg/kg; oral gavage; once daily for 16 days) reduces HBV DNA levels in the liver in a dose-dependent manner[3].
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| Animal Protocol |
Animal Model: transgenic mice that are female Tg05 transgenic mice for HBV (C57BL/6)[1]
Dosage: 5 mg/kg, 10 mg/kg Administration: Oral gavage; daily for a period of 16 days Result: For low-dose (5 mg/kg/day) and high-dose (10 mg/kg/day), the reductions in HBV DNA were 55% and 97%, respectively. |
| References |
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| Molecular Formula |
C28H52N5O5P
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|---|---|
| Molecular Weight |
569.7278
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| Exact Mass |
569.3706
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| Elemental Analysis |
C, 59.03; H, 9.20; N, 12.29; O, 14.04; P, 5.44
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| CAS # |
911208-73-6
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| Related CAS # |
202138-50-9n(fumarate);206184-49-8 (hydrate);379270-37-8n(alafenamide);206184-49-8 (hydrate);1571075-19-8n(aspartate);201341-05-1 Tenofovir dsoproxil);1236287-04-9 (Tenofovirnmaleate);1392275-56-7 (Tenofovir alafenamide hemifumarate);379270-38-9n(Tenofovir alafenamide fumarate);1453166-76-1 (Tenofovir disoproxil phosphate);1637632-97-3n(Tenofovir disoproxil succinate)
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| Appearance |
White to off-white solid powder.
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| SMILES |
C[C@@H](OCP(O)(OCCCOCCCCCCCCCCCCCCCC)=O)CN1C=NC2=C(N)N=CN=C12
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| InChi Key |
BPPMYUZIZUESBY-MLEONAHRSA-N
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| 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
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| Chemical Name |
3-(hexadecyloxy)propyl hydrogen ((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate
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| Synonyms |
Tenofovir exalidex; HDP-Tenofovir; Tenofovir; CMX-157; CMX157; CMX 157
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~175.52 mM）
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7552 mL | 8.7761 mL | 17.5522 mL | |
| 5 mM | 0.3510 mL | 1.7552 mL | 3.5104 mL | |
| 10 mM | 0.1755 mL | 0.8776 mL | 1.7552 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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