Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].

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

Hexyl-6-lactone is an ε-lactone in which the oxane is substituted with a carbonyl group at the 2-position. See also: Polycaprolactone 25 (monomer); Polycaprolactone 90 (monomer); Polycaprolactone (note moved to). Mechanism of Action: Caprolactone inhibits the proteolytic and fibrinolytic activity of human plasma proteases. At very low concentrations, it also inhibits plasminogen activation via plasmin-streptokinase activator and human urokinase. Therapeutic Uses: This article describes a method for incorporating estradiol into a biodegradable, waxy copolyester. This copolyester, prepared by direct copolymerization condensation of ε-caprolactone and δ-valerolactone under catalyst-free conditions, can be used as a matrix for implantable drug delivery systems. In vivo performance was evaluated by implanting the device into the back of male rats. Compared to homopolymers, this copolyester is more readily eroded, and the degradation of homopolymers is further accelerated by the action of lipases. Although a burst release occurred initially, drug release remained stable throughout the 19-week experimental period (week 1 to week 20). In this study, the drug release pattern paralleled the degradation pattern, indicating that drug release is the rate-limiting step in polymer degradation. Results showed that approximately 75% of the initial drug content was retained in the device 20 weeks after implantation. This finding suggests that biodegradable poly(ε-caprolactone-co-δ-valerolactone) wax can be used as an implant matrix for drug delivery systems that can control drug release over a relatively long period. The in vivo activity of the drug was confirmed by observing atrophy of the seminal vesicles and ventral prostate in male rats 10 weeks after implantation.
The release of levonorgestrel over 5 menstrual cycles after subcutaneous implantation of poly(ε-caprolactone) capsules was studied in 8 women. Except for one subject, all subjects experienced ovulation suppression during the capsule implantation period (one cycle). The capsule contained 16 mg of the drug and 61 mg of ethyl oleate (as a suspension). The serum concentration range of the drug was wide. When the serum drug concentration reaches or exceeds 300 pg/ml, it appears to inhibit ovulation.

C6H4D6O2

120.18

120.105

1219802-08-0

24980-41-4

10401

Typically exists as solid at room temperature

1.0±0.1 g/cm3

225.4±8.0 °C at 760 mmHg

-1.5 °C

109.4±0.0 °C

0.1±0.4 mmHg at 25°C

1.439

0.36

0

2

0

8

88.5

0

C1(OCCC([2H])([2H])C([2H])([2H])C1([2H])[2H])=O

PAPBSGBWRJIAAV-UHFFFAOYSA-N

InChI=1S/C6H10O2/c7-6-4-2-1-3-5-8-6/h1-5H2

oxepan-2-one

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)

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.

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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).

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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)

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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).

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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

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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.

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