57-66-9 Probenecid

Superiority:

Product Name: Probenecid
Synonyms: robenecid;Synergid R;synergidr;Tubophan;Uricosid;LABOTEST-BB LT00772250;AKOS BBS-00002773;4-(DI-N-PROPYLAMINO)SULFONYL BENZOIC ACID
CAS: 57-66-9
MF: C13H19NO4S
MW: 285.36
EINECS: 200-344-3
Product Categories: anti-gout;Miscellaneous;API;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;API's;Vanilloid/TRPV channel;chemical additive;pharmaceutical intermediate;PROBENEMID;pharmaceutical chemicals;Pharmaceutical raw materials
Mol File: 57-66-9.mol

Probenecid Chemical Properties
Melting point  194-196°C
Boiling point  438.0±47.0 °C(Predicted)
density  1.2483 (rough estimate)
refractive index  1.6800 (estimate)
storage temp.  Store at RT
form  neat
pka 5.8(at 25℃)
Water Solubility  <0.1 g/100 mL at 20 ºC
Merck  14,7754
Stability: Stable, but may be light sensitive. Incompatible with strong oxidizing agents.
CAS DataBase Reference 57-66-9(CAS DataBase Reference)
NIST Chemistry Reference P-(dipropylsulfamoyl) benzoic acid(57-66-9)
EPA Substance Registry System Probenecid (57-66-9)
Safety Information
Hazard Codes  Xn
Risk Statements  22-40
Safety Statements  36/37-24/25
RIDADR  3249
WGK Germany  3
RTECS  DG9400000
TSCA  Yes
HS Code  29350090
Hazardous Substances Data 57-66-9(Hazardous Substances Data)

Probenecid Usage And Synthesis
Anti-gout drug Probenecid is a chemically synthetic sulfa anti-gout drug, also known as oxybenzone sulfonamides, which has dual role of both promoting the excretion of uric acid excretion and inhibiting the excretion of penicillin. Clinically it is used for treating chronic gout and suppressing excretion of penicillin-type drugs in order to increase their clinical plasma concentration as an adjuvant drug of penicillin therapy. Its mechanism of action is inhibiting the re-absorption of renal tubular on uric acid, thus increasing uric acid excretion and further lowering plasma uric acid concentration for reducing the deposition of urate in tissues and prevent the crystallization of urate. This product can also promote the dissolution of the pre-formed urate, thereby reducing its damage on the joint. In addition, the product can also competitively inhibit the secretion of a weak organic acid (such as penicillin, cephalosporins) in the renal tubules, which can increase blood concentrations of these antibiotics and prolong their duration of action. This product is easy for oral administration with a plasma protein binding rate of 85% to 90%. Adults take 1 g orally each time with the plasma concentration reaches peak after 2~4 hour and with a half-life of being 6 to 12 hours. Probenecid is rapidly metabolized in the liver with the major metabolite being probenecid acetyl glucuronic acid. The main metabolite is excreted through the urine. This product has no anti-inflammatory and analgesic effect, and thus being invalid for treating acute gout. Acute toxicity test results: orally: LD50 of rats being 1600mg/kg. After the oral administration, the major adverse reactions are gastrointestinal reactions with others adverse reactions including dizziness, headache, facial flushing, urinary frequency, gingival swelling and pain, skin rash; there are also occasional allergic reactions. It is not suitable for being applied to patients of acute gout and with history of uric acid crystal deposition in kidney and ureter. Patients of peptic ulcer or blood abnormalities and pregnant women should take with caution. Patients of renal dysfunction are not allowed for using it.