Olaquindox (100 mg/kg in the baseline diet) raises the feed conversion ratio (FCR) and average daily growth [1].

Absorption, Distribution and Excretion
Experiments with (3-1)4C-olaquindox intraduodenally administered to rats with bile duct fistulas suggested that around 18% of the dose was excreted in the bile. Similar findings were made after intravenous dosing. Distribution occurred in a generalized manner throughout the body after oral dosing and most of the radioactivity had disappeared by 24 hours. Autoradiography revealed the highest amount in the rat kidney at 4 hours, indicative of the extent of urinary excretion already noted. Slightly elevated concentrations were also observed in liver, testes, adrenals and hair follicles.
After pigs were given diets containing up to 45 ppm olaquindox for the duration of the fattening period, the highest levels were found in the liver (0.14 ppm) and kidney (0.28 ppm) 6 hours after withdrawal. By 24 hours the levels were below the limit of detection (0.1 ppm). Similar results were noted when pigs were given diets containing 10 ppm olaquindox.
When pigs were dosed at levels in the range of those recommended in use (up to 100 ppm in the diet) for up to 20 weeks, relatively high levels were found in the kidney (around 2000 ppb) with relatively moderate levels in the liver (300 ppb) when the animals were killed six hours after drug withdrawal. When killed 2 days after withdrawal, levels had fallen to below the limits of detection (50 ppb) in liver, kidney and muscle. Pigs given diets containing olaquindox at levels in excess of those recommended (160 or 250 ppm) for up to 4 weeks also had high initial levels in kidney, liver and muscle but these had fallen to below the limits of detection by day 2 after withdrawal.
Olaquindox was rapidly absorbed when given orally to pigs. Over 90% of an oral dose of 2 mg/kg bw was eliminated in the urine within 24 hours, which is indicative of rapid and extensive absorption. The remainder was excreted in the feces. Maximum plasma levels were attained within 1-2 hours of dosing (1-2 ppm). This was followed by a rapid decline in plasma levels reaching around 0.03 ppm by 24 hours and 0.005-0.01 ppm by 48 hours. Radioactivity was present in all tissues when examined 2 days after dosing, but the levels were extremely low. In the kidney and liver, levels of 110 and 52 ppb were found, while levels in muscle were only 9 ppb. After 8 days, levels in liver and kidney had fallen to 27 and 12 ppb, respectively, while those in muscle were in the range of 2.5 ppb. By 28 days after dosing only low levels were found in kidney and muscle (0.9 and 0.5-0.8 ppb, respectively) with slightly higher concentrations in the liver (2 ppb).
For more Absorption, Distribution and Excretion (Complete) data for OLAQUINDOX (6 total), please visit the HSDB record page.

---

Metabolism / Metabolites
The biotransformation of olaquindox has been investigated only in the pig. The majority of an oral dose of olaquindox (70%) was excreted in the urine unchanged. The major metabolites appeared to be the reduced compounds, the 1- or 4-mono-N-oxides (16%). Three other compounds thought to be carboxylic acid derivatives made up the remainder. Later work led to the elucidation of the structures of these metabolites in the pig. Again the major urinary component after oral dosing was olaquindox with about 7% present as the 4-mono-N-oxide. Omega oxidation produced the 2-carboxymethylaminocarbonyl compound and its 4-mono-N-oxide derivative (6%). Some of the corresponding 1-mono-N-oxide moiety of the 2-carboxymethylaminocarbonyl was also noted (1%). The remaining metabolite was the di-desoxy derivative of 2-carboxymethylaminocarbonyl compound, 2-carboxymethylaminocarbonyl-3- methyl quinoxaline (>1%).

[1]. Ding MX, et al. Olaquindox and cyadox stimulate growth and decrease intestinal mucosal immunityof piglets orally inoculated with Escherichia coli. J Anim Physiol Anim Nutr (Berl). 2006 Jun;90(5-6):238-43.

Olaquindox [BAN:INN] is a quinoxaline derivative.

C12H13N3O4

263.2493

263.09

23696-28-8

Olaquindox-d4;1189487-82-8

71905

Pale yellow crystals

1.4±0.1 g/cm3

343.3ºC

209°C (dec.)

>204.4ºC

1.651

-2.2

2

5

3

19

421

0

O=[N+]1C2=C([H])C([H])=C([H])C([H])=C2N(C(C([H])([H])[H])=C1C(N([H])C([H])([H])C([H])([H])O[H])=O)[O-]

TURHTASYUMWZCC-UHFFFAOYSA-N

InChI=1S/C12H13N3O4/c1-8-11(12(17)13-6-7-16)15(19)10-5-3-2-4-9(10)14(8)18/h2-5,16H,6-7H2,1H3,(H,13,17)

N-(2-hydroxyethyl)-3-methyl-4-oxido-1-oxoquinoxalin-1-ium-2-carboxamide

Bisergon; Bayonox; Bayernox

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

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

DMSO : ~25 mg/mL (~94.97 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

---

Solubility in Formulation 2: ≥ 2.5 mg/mL (9.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

---

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