G-28315, also known as SuLfinpyrazone, increases fibrinolytic action [2].

At an oral dose of 30 mg/kg, SuLfinpyrazone (G-28315) was able to dramatically delay the euglobulin clot lysis time in rats that had paw edema caused by kaolin. Apart from these benefits, rabbits were additionally shielded from rapid mortality caused by arachidonic acid by a single oral dose of 10–30 mg/kg SuLfinpyrazone [2].

Absorption, Distribution and Excretion
...WELL ABSORBED AFTER ORAL ADMIN. ...BOUND TO PLASMA PROTEINS...98-99%. T/2... IN PLASMA AFTER IV INJECTION IS ABOUT 3 HR. AFTER ORAL ADMIN...URICOSURIC EFFECT MAY PERSIST FOR...10 HR. ALTHOUGH LITTLE...IS AVAILABLE FOR FILTRATION @ GLOMERULUS, IT IS SECRETED BY PROXIMAL TUBULE & UNDERGOES LITTLE PASSIVE BACK DIFFUSION...
APPROX HALF OF ORALLY ADMIN DOSE APPEARS IN URINE WITHIN 24 HR. MOST OF DRUG (90%) IN URINE IS UNCHANGED; REMAINDER IS ELIMINATED AS...METABOLITE...
...RAPIDLY EXCRETED IN MAN, TOGETHER WITH P-HYDROXYLATED METABOLITE. PLASMA T/2...IN RATS...16.2 HR, &...18% OF IP DOSE...WAS EXCRETED INTO URINE. PLASMA T/2 IN MAN...BETWEEN 1 & 3 HR. MAIN ROUTE OF ELIMINATION IN RAT...FECES (68% OF DOSE)...CONSIDERABLE PORTION...EXCRETED IN BILE WAS REABSORBED FROM INTESTINAL TRACT.
...SULFINPYRAZONE...IS EXCRETED IN URINE OF RATS TO ONLY A SMALL EXTENT. ... CLEARED FROM CIRCULATION MAINLY THROUGH BILE...NO EVIDENCE OF ENTERO-HEPATIC CIRCULATION MECHANISM.
UNCHANGED DRUG /IN RAT/ WAS PRINCIPAL EXCRETION PRODUCT & ONLY 28%...IN URINE & 24%...IN FECES & BILE WAS FOUND AS P-HYDROXYSULFINPYRAZOLE. FAILURE OF RAT TO EXCRETE A HIGH PROPORTION OF THE DRUG IN URINE MAY BE RELATED TO ITS LACK OF URICOSURIC PROPERTIES IN THIS SPECIES.

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Metabolism / Metabolites
MOST OF DRUG (90%) IN URINE IS UNCHANGED; REMAINDER IS ELIMINATED AS N1-P-HYDROXYPHENYL METABOLITE...
.../IN RAT/ 28%...IN URINE & 24%...IN FECES & BILE WAS FOUND AS P-HYDROXYSULFINPYRAZOLE.
Sulfinpyrazone has known human metabolites that include Sulfinpyrazone sulfone.
Sulfinpyrazone is a known human metabolite of sulfinpyrazone_sulfide.

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Biological Half-Life
Approximately 4-6 hours

Protein Binding
98-99%

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Interactions
...URICOSURIC ACTION /OF SULFINPYRAZONE/ IS ADDITIVE TO THAT OF PROBENECID & PHENYLBUTAZONE BUT IS MUTUALLY ANTAGONISTIC TO THAT OF SALICYLATES. ... POSSESSES ABILITY TO DISPLACE OTHER ORG ANIONS THAT ARE BOUND EXTENSIVELY TO PLASMA PROTEINS...THUS ALTERING THEIR DISTRIBUTION TO TISSUES & THEIR RENAL EXCRETION...
...SULFINPYRAZONE MAY POTENTIATE ACTIONS OF INSULIN & ORAL HYPOGLYCEMIC AGENTS...
SULFINPYRAZONE MAY DISPLACE SULFONAMIDES FROM PLASMA PROTEIN BINDING SITES...

[1]. Margulies EH, White AM, Sherry S. Sulfinpyrazone: a review of its pharmacological properties and therapeutic use. Drugs. 1980;20(3):179‐197.

[2]. Rüegg M. Antithrombotic effects of sulfinpyrazone in animals: influence on fibrinolysis and sodium arachidonate-induced pulmonary embolism. Pharmacology. 1976;14(6):522‐536.

Sulfinpyrazone is a sulfoxide and a member of pyrazolidines. It has a role as a uricosuric drug.
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.
Sulfinpyrazone is a phenylbutazone derivative with uricosuric and antithrombotic properties. Sulfinpyrazone competitively inhibits reabsorption of urate at the proximal renal tubule in the kidney. This agent acts on the organic anion transport exchanger, thereby increasing uric acid excretion and decreasing serum uric acid levels resulting in the prevention of urate deposition. Sulfinpyrazone also blocks tubular excretion of various acidic drugs, resulting in increased serum concentration of the drugs. In addition, sulfinpyrazone and its active metabolite inhibit the synthesis of thromboxane A2, by competitively inhibiting the activity of cyclooxygenase, thereby preventing platelet aggregation through restoration of platelet survival time to normal, and decreasing platelet adhesiveness to subendothelial cells.
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.

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Drug Indication
For the treatment of gout and gouty arthritis.

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Mechanism of Action
Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs).
...IN SUFFICIENT DOSAGE IS POTENT INHIBITOR OF RENAL TUBULAR REABSORPTION OF URIC ACID. ...SMALL DOSES MAY REDUCE EXCRETION...PRESUMABLY BY INHIBITING SECRETORY BUT NOT REABSORPTIVE TRANSPORT. BY COMPETITIVE INHIBITION...REDUCES RENAL TUBULAR SECRETION OF OTHER ORG ANIONS...AS PAH /PARA-AMINOHIPPURIC/ & SALICYLIC ACID.

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Therapeutic Uses
Uricosuric Agents
EXPTL USE: SULFINPYRAZONE...PROLONGS PLATELET SURVIVAL IN MAN. ...BLOCK PLATELET AGGREGATION IN RESPONSE TO COLLAGEN & ANTIGEN-ANTIBODY COMPLEXES BUT NOT IN RESPONSE TO ADP OR THROMBIN...APPEARS RELATED TO DIMINISHED RELEASE OF ADP & 5-HYDROXYTRYPTAMINE. ...BEING STUDIED FOR...PROPHYLACTIVE VALUE IN THROMBOEMBOLIC DISORDERS
SULFINPYRAZONE USP...AS OFFICIAL 100-MG TABLETS & 200 MG CAPSULES. FOR... CHRONIC GOUT, INITIAL DOSAGE IS 100-200 MG/DAY. AFTER 1ST WK, DOSE...GRADUALLY INCR UNTIL SATISFACTORY LOWERING OF PLASMA URIC ACID IS ACHIEVED & MAINTAINED...MAY REQUIRE FROM 100-400 MG/DAY, DIVIDED INTO 2-4 DOSES & PREFERABLY GIVEN WITH MEALS.
OCCASIONAL RESISTANT PT HAVE BEEN TREATED SUCCESSFULLY WITH DOSES AS HIGH AS 800 MG/DAY. LARGER DOSES ARE POORLY TOLERATED & UNLIKELY TO PRODUCE FURTHER URICOSURIC EFFECT IN RESISTANT PT. IN RESPONSIVE PT...SINGLE DAILY DOSE OF 100 MG IS SOMETIMES SATISFACTORY FOR MAINTENANCE.
For more Therapeutic Uses (Complete) data for SULFINPYRAZONE (10 total), please visit the HSDB record page.

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Drug Warnings
SULFINPYRAZONE LACKS CLINICALLY-STRIKING ANTI-INFLAMMATORY & ANALGESIC PROPERTIES OF ITS CONGENER, PHENYLBUTAZONE.
GI IRRITATION OCCURS IN 10-15% OF ALL PT...AN OCCASIONAL PT MAY REQUIRE DISCONTINUANCE OF ITS USE. FREQUENCY & SEVERITY INCR WITH DOSAGE...DISTRESS IS LESSENED WHEN DRUG IS TAKEN IN DIVIDED DOSES WITH MEALS. ...GIVEN TO PT WITH HISTORY OF PEPTIC ULCER ONLY WITH GREATEST CAUTION & CAREFUL OBSERVATION.
...ABILITY OF DRUG TO DEPRESS HEMATOPOIESIS HAS BEEN DEMONSTRATED...PERIODIC BLOOD-CELL COUNTS ARE THEREFORE ADVISED DURING PROLONGED THERAPY. ADEQUATE PRECAUTIONS MUST ALSO BE TAKEN TO PREVENT INTRARENAL PPTN OF URATES...
IN CLINICAL USE OF...URICOSURIC DRUGS, IT MUST BE KEPT IN MIND THAT THEY CAN ALTER PLASMA BINDING, DISTRIBUTION, & RENAL EXCRETION OF OTHER ORG ACIDS... WHETHER THESE BE NATURALLY OCCURRING...OR DRUGS & DRUG METABOLITES. /URICOSURICS/
For more Drug Warnings (Complete) data for SULFINPYRAZONE (8 total), please visit the HSDB record page.

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Pharmacodynamics
Sulfinpyrazone's pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.

C23H20N2O3S

404.4815

404.119

57-96-5

5342

White to off-white solid powder

1.4±0.1 g/cm3

590.8±42.0 °C at 760 mmHg

>300 °C(lit.)

311.1±27.9 °C

0.0±1.7 mmHg at 25°C

1.717

2.3

0

4

6

29

571

0

MBGGBVCUIVRRBF-UHFFFAOYSA-N

InChI=1S/C23H20N2O3S/c26-22-21(16-17-29(28)20-14-8-3-9-15-20)23(27)25(19-12-6-2-7-13-19)24(22)18-10-4-1-5-11-18/h1-15,21H,16-17H2

1,2-diphenyl-4-(2-(phenylsulfinyl)ethyl)pyrazolidine-3,5-dione

G-28315; G28315; G 28315; Sulfinpyrazone; Anturane; Anturanil

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)

DMSO : ~33.33 mg/mL (~82.40 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: 2.5 mg/mL (6.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.18 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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