Sulfamoxole
(Synonyms: 磺胺二甲唑) 目录号 : GC45610
A sulfonamide antibiotic
Cas No.:729-99-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sulfamoxole is a sulfonamide antibiotic.1 It is inactive or weakly active against bacteria when used alone but acts synergistically with trimethoprim against a variety of bacteria in vitro, including strains of S. pyogenes, E. coli, and P. vulgaris when used at concentrations of 1.95-7.8, 0.12-1.95, and 0.48-0.97 μg/ml, respectively. Sulfamoxole, in combination with trimethoprim, is effective in mouse models of E. coli or P. vulgaris infection. It inhibits P. carinii recombinant dihydropteroate synthase (DHPS), an enzyme required for the biosynthesis of folate, with an IC50 value of 0.089 μM.2
|1. B•hni, E. Bacteriostatic and bactericidal activity of two trimethoprim-sulfonamide combinations. Chemotherapy 22(3-4), 262-273 (1976).|2. Hong, Y.-L., Hossler, P.A., Calhoun, D.H., et al. Inhibition of recombinant Pneumocystis carinii dihydropteroate synthetase by sulfa drugs. Antimicrob. Agents Chemother. 39(8), 1756-1763 (1995).
| Cas No. | 729-99-7 | SDF | |
| 别名 | 磺胺二甲唑 | ||
| Canonical SMILES | NC1=CC=C(S(NC2=NC(C)=C(C)O2)(=O)=O)C=C1 | ||
| 分子式 | C11H13N3O3S | 分子量 | 267.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7411 mL | 18.7056 mL | 37.4111 mL |
| 5 mM | 0.7482 mL | 3.7411 mL | 7.4822 mL |
| 10 mM | 0.3741 mL | 1.8706 mL | 3.7411 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[Antimicrobial action of the combined preparation Sulfamoxole/trimethoprim in vitro (author's transl)]
Arzneimittelforschung 1976;26(42):613-8.PMID:947321doi
A number of different methods were used to test the in vitro antimicrobial activity of the combination of N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (Sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim). 1. The minimum bacteriostatic inhibitory concentratiions of the Sulfamoxole/trimethoprim combination (5 + 1) (CN 3123; Nevin; Supristol) were determined for 131 gram-positive and gram-negative strains of bacteria. More than 88% of the strains tested were found to be highly sensitive to the combination (M1C 0.1-3.75 mug/ml). 2. Comparative studies with the combinations Sulfamoxole/trimethoprim and sulfamethoxazole/trimethoprim revealed no relevant differences of the M1C-values. 3. The synergistic effects of Sulfamoxole and trimethoprim can be demonstrated with the aid of the agar dilution and agar diffusion tests using various types of bacteria and different ratios of Sulfamoxole and trimethoprim. 4. Results obtained by studies on growth kinetics also demonstrate the synergistic and potentiating effect of combining Sulfamoxole with trimethoprim and bactericidal properties are achieved.
In vitro studies with combinations of Sulfamoxole and trimethoprim (co-trifamole)
Curr Med Res Opin 1982;8(2):128-33.PMID:7105824DOI:10.1185/03007998209109768.
Chequerboard studies with Sulfamoxole and trimethoprim against urinary pathogens showed that the combination was never antagonistic but usually showed little or no synergistic effect. An exception was with the inherently sulphonamide-resistant Strep. faecalis in which marked synergism (F.I.C. Index less than 0.3) was shown with all strains tested. This synergism is thought to be clinically relevant. Experiments were undertaken with a new in vitro test system to establish whether the combination of Sulfamoxole with trimethoprim will prevent the emergence of bacterial resistance. Using concentrations of the drugs attained in the blood during treatment, it was shown that trimethoprim monotherapy was likely to result in the emergence of trimethoprim-resistant pathogens, whereas treatment with Sulfamoxole and trimethoprim resulted in the elimination of the test bacteria without the emergence of resistance. Using urinary concentrations of drugs, the "urinary' pathogen was shown to be eliminated by trimethoprim alone or in combination with Sulfamoxole, without the emergence of resistant bacteria. This would not necessarily preclude the emergence of resistant bacteria in commensal sites exposed to lesser, sun-inhibitory drug concentrations.
[Toxicological investigations of the combination Sulfamoxole/trimethoprim, a new broad-spectrum chemotherapeutic (author's transl)]
Arzneimittelforschung 1976;26(42):634-43.PMID:947324doi
The chemotherapeutically effective 5:1 combination N1-(4,5-dimethyl-2-oxazolyl)-sulfanilamide (Sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) (CN 3123, Nevin, Supristol) was investigated to determine any evidence of toxicological potentiation or new toxic signs. It was found that CN 3123 had a very low acute toxicity when administered orally to mice, rats and dogs (oral LD50: mouse greater than 12 000 mg/kg; rat greater than 14 000 mg/kg; dog greater than 1000 mg/kg body weight). The combination was also tolerated by rats and dogs in repeated doses administered over a period of 4 or 26 weeks, that greatly exceeded the therapeutic dose. The only change observed occurred in the thyroid, which in all doses administered exhibited a dose-related increase in weight accompanied by histological changes indicating an activation of thyroid function and a hypersecretion of basophilic thyrotropic cells in the anterior lobe of the pituitary. Six weeks after discontinuation of treatment this condition showed a tendency to reversibility or had already returned to normal. In dogs there was a dose-related increase in iodine uptake by the thyroid and a decrease in serum thyroxine over a period of 6 months under the highest dosage of CN 3123 administered. Whereas the thyroid changes observed under the combination could be reproduced with Sulfamoxole, no effect on thyroid weight was observed in rats and dogs in the subacute toxicity phase of a comparative investigation with trimethoprim. Moreover, trimethoprim did not increase the effect of Sulfamoxole on the thyroid gland. The effect of Sulfamoxole on the thyroid is discussed in detail with a review of the literature. It can be characterized as species-specific for sulfonamides in mice, rats, rabbits and dogs but not in monkeys or in man and appears to be caused by the inhibition of the organic binding of iodine in the thyroid, whereby the predisposing factors must vary considerably from species to species. The thyroid hypertrophy observed is due to the activation of the regulatory cycle via the anterior lobe of the pituitary. The following systemic changes occurred after 600 mg CN 3123/kg, a lethal-toxic dosage and the highest administered in the study: reduced body weight, decreased food consumption leading to cachexia, slightly increased SGPT and alkaline phosphatase, slight thrombocyte depression, enlargement and increased fatty degeneration of the liver, occurrence of necrotic areas in the liver, hemosiderin accumulation in Kupffer's cells, and an increase of reticular cells in the spleen. The acute toxicity of CN 3123 and all major functional and histological changes under repeated administration were due exclusively to Sulfamoxole. The combination Sulfamoxole/trimethoprim gives no indication of toxicological potentiation or new toxic signs.
Dispersion of Sulfamoxole in tissues of poultry
Indian J Physiol Pharmacol 1977 Jan-Mar;21(1):63-5.PMID:873593doi
The blood levels and tissue dispersion of Sulfamoxole in poultry has been investigated. The clinical importance and public health hazards on the basis of the results obtained has been discussed.
[Experimental studies on the effect of the combination Sulfamoxole/trimethoprim on the Toxoplasma infection of the mouse (author's transl)]
Arzneimittelforschung 1976;26(42):620-2.PMID:947322doi
Albino mice infected with Toxoplasma gondii (virulent strain BK) were treated for 20 days with a combination of N1-[4,5-dimethyl-2-oxazolyl]-sulfanilamide (Sulfamoxole) and 2,4-diamino-5-(3,4,5-trimethoxy-benzyl)-pyrimidine (trimethoprim) in the ratio of 5:1 (trial preparation CN 3123; Nevin, Supristol). By the suitable dosage the mortality rate could be reduced considerably. In contrast to the untreated controls no antibodies were formed. No cysts could be detected in the brains of treated animals. Compared with the combination of trimethoprim/sulfamethoxazole the combination of trimethoprim/Sulfamoxole showed a slightly better effect.