| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| Other Sizes |
Purity: ≥98%
| Targets |
The target is Pneumocystis carinii dihydropteroate synthase (DHPS). No IC50, Ki, EC50 values are provided in this paper. [1]
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| ln Vitro |
Sulfamethoxypyridazine is found to be highly effective in a preliminary study of P. carinii-infected rats. Sulfamethoxypyridazine is also found to be as effective as sulfamethoxazole in P. carinii-infected rats at 1 mg/kg of body weight/day. Sulfamethoxypyridazine is effective aganist a murine model of P. carinii with ED50s of 0.06 mg/kg/day and 0.08 mg/kg/day as determined by the Giemsa and silver stain scores, respectively. Sulfamethoxypyridazine at either 0.1 mg/kg/day or 0.3 mg/kg/day is found to be significantly more effective than sulfamethoxazole at 0.47 mg/kg/day) aganist a murine model of P. carinii. Sulfamethoxypyridazine exhibits the biological half lives of 11.0 hours and 13.7 hours following im and sc administration, respectively, in goats. Sulfamethoxypyridazine exhibits the systemic availabilities of 68.6% and 58.7% following im and sc administration, respectively, in goats. Sulfamethoxypyridazine exhibits the distribution and elimination half life of 0.1 hour and 6.28 hours, respectively, in goats. Sulfamethoxypyridazine exhibits the values of apparent volume of distribution at steady state and total body clearance of 0.39 mL/kg/min and 0.73 mL/kg/min, respectively, in goats.
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| ln Vivo |
In a therapeutic protocol (3 weeks starting 3 weeks post-infection), Sulfamethoxypyridazine showed dose-dependent efficacy with calculated ED50 of 0.06 mg/kg/day (by Giemsa stain) and 0.08 mg/kg/day (by silver stain), and ED90 of 0.17-0.19 mg/kg/day. [1]
In a prophylactic protocol (6 weeks starting 1 day post-infection), the ED50 was 0.03 mg/kg/day and ED90 was 0.11-0.12 mg/kg/day. [1] At doses of 0.1 or 0.3 mg/kg/day, Sulfamethoxypyridazine was significantly more effective than sulfamethoxazole at 0.18, 0.25, or 0.47 mg/kg/day (P<0.01). [1] Giemsa and silver stain scores for infection intensity were reduced from control averages of 4.38 and 3.45 respectively to near zero at effective doses. [1] |
| Animal Protocol |
BALB/c mice were transtracheally infected with Pneumocystis carinii. Sulfamethoxypyridazine was administered via drinking water daily. For the therapeutic protocol, treatment began 3 weeks after infection and continued for 3 weeks. For the prophylactic protocol, treatment began 1 day after infection and continued for 6 weeks. Each treatment group consisted of 10 mice. At the end of treatment, mice were sacrificed and infection intensity was assessed on Giemsa-stained slides (for trophozoites) and silver-stained slides (for cysts). Scores ranged from 0 (no organisms in 50 × 1000× microscopic fields) to 5 (>100 organisms per 1000× field). Scores were determined by two microscopists in a blinded manner and then averaged. [1]
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| ADME/Pharmacokinetics |
The half-life of Sulfamethoxypyridazine is 37 hours in humans and 13 hours in rats. Half-life in mice has not been measured but is presumed to be substantially longer than that of sulfamethoxazole. [1]
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| Toxicity/Toxicokinetics |
Sulfamethoxypyridazine is considered likely to be safe based on data from Sulfapral (a combination of sulfamethizole and SMPR), which had the lowest fatality rate and second-lowest serious reaction rate among nine sulfa drugs analyzed at a daily dose of approximately 6 mg/kg in humans. [1]
However, Sulfamethoxypyridazine can cause severe adverse effects such as Stevens-Johnson syndrome, though there is no evidence that such effects are more common than with sulfamethoxazole. [1] Patients allergic to sulfamethoxazole are unlikely to tolerate Sulfamethoxypyridazine due to structural similarity. [1] |
| References |
Antimicrob Agents Chemother.1998 Apr;42(4):934-5;VetRes.1997;28(1):101-4.
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| Additional Infomation |
Sulfamethoxypyridazine is a sulfonamide drug composed of a methoxy substituent on the pyridazine ring and a 4-aminobenzenesulfonamide group at the 3-position. It has anti-infective, EC 2.5.1.15 (dihydropteranoic acid synthase) inhibitory, and anti-allergic effects. It belongs to the pyridazine, sulfonamide, and sulfonamide antibiotic classes. Its function is related to sulfonamide drugs. Sulfamethoxypyridazine is a long-acting sulfonamide antibiotic. It is a sulfonamide antibacterial agent.
Sulfamethoxypyridazine might be considered as an alternative to trimethoprim-sulfamethoxazole for prophylaxis and treatment of Pneumocystis carinii pneumonia because it has a longer half-life allowing less frequent dosing, and by using a sulfa drug without trimethoprim, adverse effects due to trimethoprim can be avoided. [1] Concerns include potential cross-allergy with other sulfa drugs, risk of Stevens-Johnson syndrome, and emerging sulfa-resistant P. carinii strains. [1] |
| Molecular Formula |
C11H12N4O3S
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| Molecular Weight |
280.3
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| Exact Mass |
280.063
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| CAS # |
80-35-3
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| Related CAS # |
Sulfamethoxypyridazine-d3;1172846-03-5
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| PubChem CID |
5330
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
564.9±60.0 °C at 760 mmHg
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| Melting Point |
182 °C
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| Flash Point |
295.4±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.647
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| LogP |
0.32
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
376
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VLYWMPOKSSWJAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12N4O3S/c1-18-11-7-6-10(13-14-11)15-19(16,17)9-4-2-8(12)3-5-9/h2-7H,12H2,1H3,(H,13,15
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| Chemical Name |
Benzenesulfonamide, 4-amino-N-(6-methoxy-3-pyridazinyl)-
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5676 mL | 17.8380 mL | 35.6761 mL | |
| 5 mM | 0.7135 mL | 3.5676 mL | 7.1352 mL | |
| 10 mM | 0.3568 mL | 1.7838 mL | 3.5676 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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