Interactions
The following drugs may enhance the response to Coumafuryl or indanedione derivatives: alcohol (acute poisoning), allopurinol, aminosalicylic acid, amiodarone, anabolic steroids, chloral hydrate, chloramphenicol, cimetidine, clofibrate, trimethoprim-sulfamethoxazole, danazol, dexthylexin sodium, diazoxide, diflunisal, disulfiram, erythromycin, ethacrynic acid, fenoprofen calcium, glucagon, ibuprofen, indomethacin, influenza vaccine, isoniazid, meclofenamic acid, mefenamic acid, methylthiouracil, metronidazole, miconazole, nalidixic acid, neomycin (oral), pentoxifylline, phenylbutazone, propoxyphene, propylthiouracil, quinidine, quinine. Salicylates, streptokinase, sulfinpyrazone, sulfonamides, sulindac, tetracyclines, thiazide diuretics, thyroid medications, tricyclic antidepressants, urokinase, vitamin E. /Coumafuryls and Indanedione Derivatives/
The following drugs...may...reduce...the response to Coumafuryl or indanedione derivatives: alcohol (chronic alcoholism), barbiturates, carbamazepine, corticosteroids, adrenocorticotropic hormone, ethylclofenac, glutamine, griseofulvin, mercaptopurine, methylquinone, estrogen-containing oral contraceptives, rifampin, spironolactone, vitamin K. /Coumafuryls and Indanedione Derivatives/

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Non-human toxicity values
LD50: Rat (Norwegian albino rat) oral administration 900.0 mg/kg

Coumachlor is a hydroxyCoumafuryl. Mechanism of Action 4-HydroxyCoumafuryl derivatives and indanedione (also known as oral anticoagulants) are both vitamin K antagonists. Their use as rodenticides works by inhibiting vitamin K-dependent steps in the synthesis of various blood coagulation factors. Vitamin K-dependent proteins involved in the coagulation cascade (Figure 1) include procoagulant factors II (prothrombin), VII (prothrombin convertase), IX (Christmas factor), and X (Stuart-Proll factor), as well as coagulation inhibitory proteins C and S. All of these proteins are synthesized in the liver. Before being released into the bloodstream, various precursor proteins undergo numerous (intracellular) post-translational modifications. Vitamin K acts as a coenzyme in one of these modifications, specifically by carboxylating 10-12 glutamate residues at a specific site to generate γ-carboxyglutamate (Gla). The presence of these Gla residues is crucial for the procoagulant activity of various coagulation factors. Vitamin K hydroquinone (KH2) is an active coenzyme that is oxidized to vitamin K 2,3-epoxide (KO), providing the energy required for the carboxylation reaction. Subsequently, this epoxide is recycled through two reduction steps catalyzed by KO reductase (Figure 2). KO reductase is the target of Coumafuryl anticoagulants. Inhibition of KO reductase by Coumafuryl anticoagulants leads to rapid depletion of KH2, effectively preventing the formation of Gla residues. This results in the accumulation of uncarboxylated clotting factor precursors in the liver. In some cases, these precursor proteins are further processed without carboxylation and (depending on the species) may appear in the bloodstream. At this point, the uncarboxylated protein is called a decarboxylated clotting factor. Normal clotting factors circulate as proenzymes, which can only be activated after limited proteolytic degradation to participate in the coagulation cascade. Decarboxylated clotting factors do not have procoagulant activity (i.e., cannot be activated) and cannot be converted into active proenzymes by the action of vitamin K. While high levels of circulating decarboxylation clotting factors can be detected in humans receiving anticoagulation therapy, these levels are negligible in rats and mice treated with warfarin. /Anticoagulant rodenticide/
Similar to warfarin, it delays the effect on prothrombin levels and blood clotting, ultimately leading to bleeding death.

C19H15CLO4

342.77

342.065

81-82-3

54682651

Colorless, crystalline solid
Crystals

1.4±0.1 g/cm3

543.1±50.0 °C at 760 mmHg

168-170 °C(lit.)

282.3±30.1 °C

0.0±1.5 mmHg at 25°C

1.641

4.01

1

4

4

24

534

0

O=C1C(C(CC(C)=O)C2C=CC(Cl)=CC=2)=C(O)C2C(=CC=CC=2)O1

DEKWZWCFHUABHE-UHFFFAOYSA-N

InChI=1S/C19H15ClO4/c1-11(21)10-15(12-6-8-13(20)9-7-12)17-18(22)14-4-2-3-5-16(14)24-19(17)23/h2-9,15,22H,10H2,1H3

3-[1-(4-chlorophenyl)-3-oxobutyl]-4-hydroxychromen-2-one

G 23133; G-23133; Coumachlor

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.)