Absorption, Distribution and Excretion
Most organophosphorus compounds…are absorbed through the skin, conjunctiva, gastrointestinal tract, and lungs. /Organophosphorus compounds/
The skin absorption rate of organophosphorus pesticides can be affected by the solvent used. /Organophosphorus pesticides/
Many organophosphorus insecticides are excreted in latex. /Organophosphorus insecticides/
After absorption, almost all organophosphorus compounds are excreted in urine as hydrolysis products. /Anticholinesterase agents/
For more complete data on the absorption, distribution, and excretion of chlorothiophosphates (7 in total), please visit the HSDB records page.

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Metabolism/Metabolites
Degrades rapidly in plants and animals, with metabolites including sulfoxides and sulfones.
Plasma and tissue enzymes are responsible for hydrolyzing organophosphorus compounds into their corresponding phosphates and phosphonates. However, oxidases are also involved in the metabolism of some organophosphorus compounds. /Anticholinesterase agents/
Organophosphorus anticholinesterase agents are hydrolyzed in vivo by a group of enzymes called A-esterases or paraoxonases. These enzymes are present in blood plasma and liver, and hydrolyze large amounts of organophosphate compounds by cleaving phosphate ester bonds, acid anhydride bonds, PF bonds, or P-CN bonds. Anticholinesterase agents.

Interactions
Some phenothiazines may antagonize or enhance the toxic anticholinesterase effects of organophosphate pesticides and organophosphate cholinesterase inhibitors. In long-term treatment, corticosteroids may antagonize the anti-glaucoma effect (increased intraocular pressure) of anticholinesterase. …Anticholinergic drugs may antagonize the miotic (anti-glaucoma) effects of anticholinesterase on the autonomic and central nervous systems, as well as other muscarinic effects. Tricyclic antidepressants (which have anticholinergic effects) may antagonize the anti-glaucoma (miotic) effect of anticholinesterase in glaucoma. …Antihistamines with anticholinergic effects may antagonize the miotic (anti-glaucoma) and central nervous system effects of anticholinesterase. Anticholinesterase may enhance the sedation and behavioral changes induced by antihistamines. The effects of anticholinesterase drugs on autonomic nerve effector cells, and to some extent on the central nervous system, can be antagonized by atropine, which is the first-line antidote. The effects of barbiturates can be enhanced by anticholinesterases. ... Dextropanol can enhance the effects of anticholinesterases. Fluorophosphates can enhance the effects of other anticholinesterases. /Anticholinesterase/
The effects of barbiturates can be enhanced by anticholinesterases. Although barbiturates can be used with caution to treat convulsions, extreme caution must be exercised when treating anticholinesterase poisoning (especially organophosphate poisoning). Echothion is a cholinesterase inhibitor used as a mitogen; it can enhance the effects of other cholinesterase inhibitors used for other purposes (additive effect) or may produce a synergistic effect. Personnel exposed to organophosphate pesticides must take strict precautions. ...Organophosphate pesticides: have additive anticholinesterase effects. Danger. Patients using anticholinesterase medications (even topical medications, such as eye drops) should avoid areas where organophosphate pesticides have been recently used. /Anticholinesterase/
Anticholinesterase (organophosphate) pesticides antagonize polarized muscle relaxants. Phenothiazines/and thioxanthates/: ...may enhance the toxic effects of organophosphate pesticides. /Organophosphate pesticides/

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Non-human toxicity values
Oral LD50 in rats: 9.1 mg/kg /tech grade/
Oral LD50 in mice: 91.4 mg/kg /tech grade/
Subcutaneous LD50 in rabbits: 31 mg/kg /tech grade/
Oral LD50 in male rats = 10.7 mg/kg, oral LD50 in female rats = 7.8 mg/kg
For more (complete) non-human toxicity values for Chlorthiophos (9 in total), please visit the HSDB records page.

Chlorthiophos is a yellowish-brown liquid that crystallizes readily below 77°F (25°C). It is used as an insecticide and acaricide. (EPA, 1998) Chlorthiophos is an organothiophosphate. Mechanism of Action: Symptoms of organophosphate poisoning are caused by the accumulation of acetylcholine, leading to excessive excitation of the parasympathetic nervous system. Symptoms are generally classified into three categories: muscarinic, nicotinic, and central nervous system symptoms. Muscarinic symptoms include salivation, lacrimation, sweating, and runny nose. Other symptoms include constricted pupils, difficulty breathing, vomiting, diarrhea, and frequent urination. Nicotinic effects include muscle tremors, weakness, and paralysis. Central nervous system symptoms include tension, anxiety, ataxia, convulsions, and coma. Death is usually caused by respiratory failure, but sometimes by cardiac arrest. Symptoms vary little among different organophosphates, but the absorption pathway may have a greater impact on certain systems. /Organophosphorus Compounds/
The characteristic pharmacological action of anticholinesterase drugs is primarily attributed to their inhibition of the hydrolysis of acetylcholinesterase (ACh) by acetylcholinesterase (AChE) at cholinergic transmission sites. Consequently, neurotransmitters accumulate, and the response of ACh released by cholinergic impulses or spontaneously released at nerve endings is enhanced. Most organophosphorus drugs…almost all acute effects at moderate doses are attributed to this action. /Antochlinesterase Drugs/
The cardiovascular effects of anticholinesterase drugs are complex, as they reflect the intraganglionic and postganglionic effects of accumulated ACh on the heart and blood vessels. The primary peripheral effect of accumulated ACh on the heart is bradycardia, leading to a decrease in cardiac output. Higher doses typically result in a decrease in blood pressure, usually due to the effects of anticholinesterase drugs on the medullary vasomotor center of the central nervous system. /Antochlinesterase Drugs/
Organophosphorus derivatives exert their effects by binding to and inactivating acetylcholinesterase. ...Cholinesterase inhibitor pesticides inactivate cholinesterase, leading to the accumulation of large amounts of acetylcholine, thus producing a wide range of effects, which can be divided into four categories: (1) Enhancement of postganglionic parasympathetic nerve activity. ... (2) Continuous depolarization of skeletal muscle ... (3) Initial stimulation after central nervous system cell inhibition ... (4) Varying degrees of ganglion stimulation or blockade ... /Cholinesterase inhibitor pesticides/
For more complete data on the mechanisms of action of Chlorthiophos (7 types), please visit the HSDB record page.

C11H15CL2O3PS2

361.23

359.958

21923-23-9

30859

Brown liquid with crystals at low temp

1.38

6.042

0

5

7

19

312

0

CCOP(OC1=CC(Cl)=C(SC)C=C1Cl)(=S)OCC

JAZJVWLGNLCNDD-UHFFFAOYSA-N

InChI=1S/C11H15Cl2O3PS2/c1-4-14-17(18,15-5-2)16-10-6-9(13)11(19-3)7-8(10)12/h6-7H,4-5H2,1-3H3

(2,5-dichloro-4-methylsulfanylphenoxy)-diethoxy-sulfanylidene-λ5-phosphane

S 2957; Celathion; Chlorthiophos

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.

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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.)