Absorption, Distribution and Excretion
Fry and juvenile trout were exposed to cyclic UL-14C-toluenesulfonyl chloride sodium (93.7% purity, specific activity 1.2 μCi/μM) at a concentration of 20 mg/L (twice the therapeutic concentration) for a maximum of 1 hour, followed by recovery in freshwater to assess the accumulation and distribution of residues in tissues. Well water temperatures ranged from 11.6 to 12.2 °C. The estimated half-life of p-toluenesulfonamide equivalent in fry was 27.3 hours, while the half-life of p-toluenesulfonamide residues in whole fish homogenates was 36.3 hours, determined by high-performance liquid chromatography (HPLC). Based on radiometric data, the estimated half-life of residues in juvenile fish was 32.6 hours; while the half-life of p-toluenesulfonamide residues in whole fish samples was 40.3 hours, determined by HPLC. Based on radiometric counting, the elimination rate of total sodium toluenesulfonyl chloride residues from whole-fish homogenates of fry and juveniles was rapid, but the elimination rate in fry (half-life 27.3 hours) was significantly faster than in juveniles (half-life 32.5 hours). …The absorption rate of sodium toluenesulfonyl chloride in the bath solution was very low in fry and juveniles. In this study, no sodium toluenesulfonyl chloride residues were detected in any fish tissues; only its major metabolite, p-toluenesulfonamide, was detected. Therefore, all tissue residues determined by radiometric assay or high-performance liquid chromatography (HPLC) are expressed as equivalent concentrations of p-toluenesulfonamide. Based on radiometric analysis, the equivalent concentration of p-toluenesulfonamide in the whole-fish homogenate of fry after 1 hour was 980 μg/kg, approximately 5% of the concentration in the exposed water. For juveniles, this value was 570 μg/kg, approximately 3% of the concentration in the exposed bath solution. Based on HPLC analysis, the exposure to p-toluenesulfonamide in the whole-fish homogenate of fry after 1 hour was 360 μg/kg, and for juveniles, it was 170 μg/kg.
The transdermal absorption of sodium toluenesulfonyl chloride was investigated. Five lactating cows were treated twice daily for eight days during milking. Before milking, the teats were cleaned with mammary gland tissue soaked in a 0.5% toluenesulfonyl chloride solution, and then soaked again in the solution after milking. A fresh solution containing 0.5% toluenesulfonyl chloride was prepared daily. Blood samples were collected from the jugular vein during treatment, before the last treatment, and at 30 minutes, 1 hour, 2 hours, 4 hours, 8 hours, 16 hours, and 24 hours after the last treatment. High-performance liquid chromatography (HPLC) was used to detect the toluenesulfonyl chloride in the blood before analysis, a method that hydrolyzes toluenesulfonamide before analysis. The detection limits of this method were 5 μg/kg for toluenesulfonamide and 8 μg/kg for toluenesulfonyl chloride. No residual toluenesulfonamide was detected in any of the blood samples. Therefore, it was concluded that the absorption of toluenesulfonyl chloride into the blood after transdermal teat administration is negligible.

Interactions
Studies have shown that chloramine-T can react with certain amino acids in the gastrointestinal tract to form toxic cyanide compounds. Non-human Toxicity Values Rats: Oral LD50: 935 mg/kg body weight Mice: Oral LD50: 1100 mg/kg body weight

Chloramine T is an organosodium salt derivative of toluene-4-sulfonamide, in which the amino hydrogen is replaced by chlorine. It acts as an antifouling agent, disinfectant, and sensitizer. It contains a chloro(p-toluenesulfonyl) azide compound.
See also: Chloramine T trihydrate (its active moiety).

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Mechanism of Action
/Immunoglobulin E/ is likely the mechanism by which chloramine T induces environmental or occupational asthma. /Excerpt from Table/
The major elastase inhibitors in human serum, α-1 protease inhibitors (A1PIs), are susceptible to oxidative inactivation by various substances, including chloramine T. We investigated the effects of chloramine T on the catalytic activity of porcine pancreatic elastase (PPE) and human leukocyte elastase (HLE), as well as its inhibitory effect on the elastase activity of hamster, rat, and human serum and pure human A1PIs. Both PPE and HLE were inhibited in a concentration-dependent manner by chloramine T at concentrations >0.1 mM, while trypsin was unaffected. Chloramine T inhibited the inhibitory effects of rat and human serum, as well as pure human A1PI, on PPE and HLE in a concentration-dependent manner. Conversely, chloramine T only altered the inhibitory capacity of hamster serum against HLE, without affecting its inhibitory effect on PPE. Gel size exclusion chromatography analysis revealed two major elastase inhibitory activity peaks in hamster plasma: one peak with a molecular weight of approximately 55 kDa, eluting in the A1PI region sensitive to chloramine T inactivation; and another peak with a molecular weight of approximately 180 kDa, insensitive to chloramine T. Parenteral injection of chloramine T into hamsters resulted in a slight and transient decrease in HLE inhibitory activity in serum, while a similarly slight and transient increase in PPE inhibitory activity was observed. Treatment of human erythrocyte membranes with active chlorine (…chloramine T) led to a concentration-dependent inhibition of membrane Na+, K+, and Mg2+-ATPase activities. The oxidation of thiol groups in membrane proteins coincides with enzyme inactivation and precedes the oxidation of tryptophan residues and the formation of chloramine. This study tested the hypothesis that chloramine T stimulates basal Na+ efflux from barnacle fibers, a stimulation caused by triggering Ca2+ entry from the bath into the sarcoplasm. Two explanations can be given for this. First, it is known that this oxidant can eliminate the inactivation of sodium-potassium channels. Second, L-type Ca2+ channels exist in barnacle fibers, and it is known that an increase in the concentration of free Ca2+ within these fibers leads to… (i) Chloramine T has a biphasic effect on Na+ efflux: first inhibition followed by stimulation, with a threshold concentration of 10⁻⁵ M. This concentration was also found to be the threshold concentration for shortening these fibers. … (vii) The dose-response curve of chloramine T shifts to the left in poisoned fibers. (viii) The increase in luminescence intensity depends on the extracellular Ca2+ concentration. At near-zero extracellular Ca2+ concentrations, luminescence intensity does not increase. In summary, these results support the hypothesis that chloramine-T triggers the influx of Ca2+ from the extracellular space into the sarcoplasm and provide evidence that the stimulation of Na+ efflux is not only related to this event but also to the reduction of the Na+ gradient caused by oxidative inhibition of the membrane Na+/K(+)-ATPase system. ...The effect of chloramine-T on IK1 inactivation was examined in guinea pig ventricular myocytes using patch-clamp techniques. Chloramine-T (2 mM) irreversibly inhibited the time-dependent decay of whole-cell IK1 inactivation. As a result, the negative slope region of the current-voltage (IV) relationship curve disappeared. In cell-attached single-channel recordings, the number of active channels in the patch decreased over time as the voltage was clamped to the K+ equilibrium potential (EK) -100 mV. Chloramine-T prevented this time-dependent decrease in the number of channels, and the pooled average current at EK -100 mV showed the disappearance of channel activity over time.

C7H7CLNNAO2S

227.6438

226.978

127-65-1

144-86-5 (Parent)

3641960

White or slightly yellow crystals or crystalline powder

1.36g/cm3

314.3ºC at 760mmHg

167-170 °C(lit.)

143.9ºC

3.292

0

3

1

13

231

0

Cl[N-]S(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])(=O)=O.[Na+]

VDQQXEISLMTGAB-UHFFFAOYSA-N

InChI=1S/C7H7ClNO2S.Na/c1-6-2-4-7(5-3-6)12(10,11)9-8;/h2-5H,1H3;/q-1;+1

sodium;chloro-(4-methylphenyl)sulfonylazanide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

DMSO : ~130 mg/mL (~571.08 mM)
H2O : ≥ 41 mg/mL (~180.11 mM)

Solubility in Formulation 1: ≥ 3.25 mg/mL (14.28 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 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 3.25 mg/mL (14.28 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 32.5 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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Solubility in Formulation 3: ≥ 3.25 mg/mL (14.28 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 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 100 mg/mL (439.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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