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

Absorption, Distribution and Excretion
Experiments in rats with bile duct fistulas involving intraduodenal injection of (3-1)4C-olaquindox showed that approximately 18% of the dose was excreted via bile. Similar results were observed after intravenous administration. Following oral administration, the drug was widely distributed throughout the body, with most radioactivity disappearing within 24 hours. Autoradiography showed the highest drug concentration in the rat kidneys at 4 hours, indicating urinary excretion was comparable to previously observed. Slightly elevated drug concentrations were also observed in the liver, testes, adrenal glands, and hair follicles. During the fattening period, in pigs fed diets containing up to 45 ppm olaquindox, the highest drug concentrations were observed in the liver (0.14 ppm) and kidneys (0.28 ppm) 6 hours after drug withdrawal. After 24 hours, drug concentrations were below the detection limit (0.1 ppm). Similar results were observed when pigs were fed diets containing 10 ppm olaquindox. When pigs were fed the recommended dose (maximum 100 ppm in the diet) for up to 20 weeks, and were sacrificed 6 hours after drug withdrawal, the drug concentration in the kidneys was relatively high (approximately 2000 ppb), while the drug concentration in the liver was relatively low (300 ppb). Two days after withdrawal, when sacrificed, the drug concentrations in the liver, kidneys, and muscles had all decreased to below the detection limit (50 ppb). Pigs fed a diet containing more than the recommended dose (160 or 250 ppm) of olaquindox for up to 4 weeks also had initially high drug concentrations in the kidneys, liver, and muscles, but these concentrations decreased to below the detection limit 2 days after withdrawal. Olaquindox is rapidly absorbed by pigs after oral administration. After an oral dose of 2 mg/kg body weight, over 90% is excreted in the urine within 24 hours, indicating rapid and widespread absorption. The remainder is excreted in the feces. Peak plasma concentrations (1-2 ppm) are reached within 1-2 hours after administration. Plasma concentrations subsequently decreased rapidly, reaching approximately 0.03 ppm after 24 hours and 0.005–0.01 ppm after 48 hours. Two days after administration, radioactivity was detected in all tissues, but at extremely low concentrations. Radioactivity concentrations in the kidneys and liver were 110 ppb and 52 ppb, respectively, while the concentration in muscle was only 9 ppb. After 8 days, radioactivity concentrations in the liver and kidneys decreased to 27 ppb and 12 ppb, respectively, while the concentration in muscle was approximately 2.5 ppb. At 28 days post-administration, low concentrations were detected only in the kidneys and muscle (0.9 ppb and 0.5–0.8 ppb, respectively), with a slightly higher concentration in the liver (2 ppb).
For more complete data on absorption, distribution, and excretion of olaquindos (6 types), please visit the HSDB record page.
Metabolism/Metabolites
Biotransformation of olaquindos was studied only in pigs. Following oral administration of olaquindo, the majority (70%) was excreted unchanged in the urine. The major metabolite appeared to be the reducing compound, namely 1- or 4-mono-N-oxide (16%). The remainder consisted of three compounds believed to be carboxylic acid derivatives. Subsequent studies elucidated the structure of these metabolites in pigs. Following oral administration, the major component in urine remained olaquindo, with approximately 7% present as 4-mono-N-oxide. Omega-oxidation yielded a 2-carboxymethylaminocarbonyl compound and its 4-mono-N-oxide derivative (6%). Additionally, a small amount of the corresponding 1-mono-N-oxide fraction of the 2-carboxymethylaminocarbonyl compound was detected (1%). The remaining metabolite was a dideoxy derivative of the 2-carboxymethylaminocarbonyl compound, namely 2-carboxymethylaminocarbonyl-3-methylquinoxaline (>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.

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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.

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