Diclofenac sodium structure
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Common Name | Diclofenac sodium | ||
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CAS Number | 15307-79-6 | Molecular Weight | 318.130 | |
Density | N/A | Boiling Point | 412ºC at 760 mmHg | |
Molecular Formula | C14H10Cl2NNaO2 | Melting Point | 288-290°C | |
MSDS | Chinese USA | Flash Point | 203ºC | |
Symbol |
GHS06 |
Signal Word | Danger |
Use of Diclofenac sodiumDiclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively. |
Name | diclofenac sodium |
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Synonym | More Synonyms |
Description | Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively. |
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Related Catalog | |
Target |
Human COX-2:1.3 nM (IC50, in CHO cells) Human COX-1:4 nM (IC50, in CHO cells) Ovine COX-2:0.84 μM (IC50) Ovine COX-1:5.1 μM (IC50) |
In Vitro | Diclofenac Sodium is a potent COX inhibitor, with IC50s of 4 nM and 1.3 nM for human COX-1 and COX-2 in the CHO cells, respectively. Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7 ± 3 nM[1]. Diclofenac Sodium exihibits inhibition on COX-1 and COX-2 enzyme with IC50s of 5.1 and 0.84 μM, respectively[2]. |
In Vivo | Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days[1]. Diclofenac (10 mg/kg) shows anti-inflammatory activity in mice[2]. Diclofenac (10 mg/kg) decreases oxidized low-densitylipoprotein (Ox-LDL), but shows no effects on the kinetics parameters of catalase and glutathione peroxidase via intramuscularly injection into rats[3]. |
Animal Admin | Rats[1] Male Sprague-Dawley rats (150 ± 200 g) are dosed orally with Diclofenac either once (acute dosing) or twice daily for 5 days (chronic dosing). A plasma sample is obtained 1 h after the morning dose on day 4 for measurement of Diclofenac concentration. Immediately after the administration of the last dose on day 5, the rats are injected via a tail vein with 0.5 mL of 51Cr-labelled red blood cells from a donor rat after incubation with sodium 51chromate. The rats are placed individually in metabolism cages with food and water ad libitum. Faeces are collected for a 48 h period and 51Cr faecal excretion is calculated as a % of total injected dose (20 mCi per animal)[1]. Squirrel monkeys[1] Squirrel monkeys (Saimiri sciureus; 0.8 ± 1.4 kg) are dosed orally with Diclofenac twice daily for 1 ± 5 days. One hour after administration of the last dose, 51CrCl3 in sterile saline (1 mL/kg, 4 ± 5 mCi per animal) is injected via a saphenous vein and plasma samples are obtained for measurement of Diclofenac concentration. The monkeys are then housed individually in metabolism cages. Faeces are collected for a 24 h period and 51Cr faecal excretion is calculated as a % of total injected dose[1]. |
References |
Boiling Point | 412ºC at 760 mmHg |
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Melting Point | 288-290°C |
Molecular Formula | C14H10Cl2NNaO2 |
Molecular Weight | 318.130 |
Flash Point | 203ºC |
Exact Mass | 316.998627 |
PSA | 52.16000 |
LogP | 3.10240 |
Storage condition | -20°C Freezer |
Stability | Stable. |
Water Solubility | H2O: 50 mg/mL |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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Symbol |
GHS06 |
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Signal Word | Danger |
Hazard Statements | H301 |
Precautionary Statements | P301 + P310 |
Personal Protective Equipment | Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges |
Hazard Codes | T:Toxic |
Risk Phrases | R25 |
Safety Phrases | S22-S36/37-S45 |
RIDADR | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
RTECS | AG6330000 |
Packaging Group | III |
Hazard Class | 6.1(b) |
HS Code | 2922499990 |
Precursor 9 | |
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DownStream 10 | |
HS Code | 2922499990 |
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Summary | HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0% |
Diclofenac toxicity in human intestine ex vivo is not related to the formation of intestinal metabolites.
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