Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, primarily as quantitative tracers during drug development. Studies involving the use of deuterium-labeled drugs in humans have shown that these compounds may have certain advantages over their non-deuterium-labeled counterparts. Deuterated drugs have attracted attention due to their potential to affect the pharmacokinetic and metabolic characteristics of drugs. Deuttetrabenazine is the first deuterated drug approved by the US Food and Drug Administration. Deuttetrabenazine is indicated for the treatment of chorea associated with Huntington's disease as well as tardive dyskinesia. Ongoing clinical trials indicate that many other deuterated compounds are being evaluated for use as therapeutics in humans, rather than simply as research tools. [1] Dihydroartemisinin (DHA) is an antimalarial drug. Dihydroartemisinin treatment effectively upregulates cytoplasmic RelA/p65 protein levels and downregulates nuclear RelA/p65 protein levels by blocking the nuclear translocation of RelA/p65 from the cytosol rather than inhibiting RelA/p65 protein synthesis. Dihydroartemisinin induces autophagy in RPMI 8226 cells. Dihydroartemisinin inhibits NF-κB activation in RPMI 8226 cells. The NF-κB binding activity of Dihydroartemisinin was examined by EMSA assay[3]. RPMI 8226 cells were exposed to different concentrations of Dihydroartemisinin (10, 20, and 40 μM) for 12 h, and TNF-α was introduced as a positive control for NF-κB activation. Dihydroartemisinin inhibited NF-κB activation in a dose-dependent manner compared with TNF-α[2]. Dihydroartemisinin (DHA) enhances the antitumor effect of photodynamic therapy (PDT) on esophageal cancer cells. Eca109 and Ec9706 cells were treated with Dihydroartemisinin (80 μM), PDT (25 and 20 J/cm2, respectively), or their combination. Single treatment with dihydroartemisinin or PDT resulted in a 37±5% or 34±6% decrease in Eca109 cell viability and a 33±7% or 34±6% decrease in Ec9706 cell viability, respectively. When PDT was combined with dihydroartemisinin, cell viability of the cell lines decreased by 59±6% or 61±7%, respectively[3].

Dihydroartemisinin (single oral dose; 200, 300, 400, or 600 mg/kg), given once daily on days 6-8 post infection, reduced total worm burdens by 69.2%-90.6% and female worm burdens by 62.2%-92.2%, depending on the dose in the first experiment. Similar treatments on days 34-36 post infection reduced total worm burdens by 73.9%-85.5% and female worm burdens by 83.8%-95.3%[4].

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.

[2]. Dihydroartemisinin induces autophagy by suppressing NF-κB activation. Cancer Lett. 2014 Feb 28;343(2):239-48.

[3]. Dihydroartemisinin-praziquantel combinations and multiple doses of dihydroartemisinin in the treatment of Schistosoma japonicum in experimentally infected mice. Ann Trop Med Parasitol. 2011 Jun;105(4):329-33.

[4]. Dihydroartemisinin accentuates the anti-tumor effects of photodynamic therapy via inactivation of NF-κB in Eca109 and Ec9706 esophageal cancer cells. Cell Physiol Biochem. 2014;33(5):1527-36.

C15H19D5O5

289.38

Typically exists as solid at room temperature

Dihydroqinghaosu-d5; Dihydroqinghaosu-d5; β-Dihydroartemisinin-d5; Artenimol-d5

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

---

Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

View More

Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

---

Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

View More

Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

---

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

---

 (Please use freshly prepared in vivo formulations for optimal results.)