Amprolium
(Synonyms: 氨丙啉) 目录号 : GC35328
A thiamine analog and antiprotozoal agent
Cas No.:121-25-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amprolium is a thiamine analog and antiprotozoal agent that interferes with thiamine metabolism and inhibits carbohydrate synthesis.1,2,3,4 It competitively inhibits thiamine uptake by E. tenella schizonts and by chick host intestinal cells (Kis = 7.6 and 326 μM, respectively).1 It also inhibits hexose formation and pentose utilization ex vivo in isolated lysed rat erythrocytes and in liver, kidney, heart, and intestinal tissue homogenates following dietary administration.2 Amprolium (1,000 ppm in feed) inhibits oocyst output and sporulation of Eimeria maxima, E. brunetti, and E. acervulina in infected chicks.3 It also decreases lesion and oocyst scores and mortality of E. tenella-infected chicks following dietary administration of a 125 ppm dose.4 Amprolium (100 μM) induces apoptosis in PC12 rat adrenal cells and increases the level of cleaved caspase-3.5 Formulations containing amprolium have been used as coccidiostats in poultry processing.
1.James, S.Thiamine uptake in isolated schizonts of Eimeria tenella and the inhibitory effects of amproliumParasitology80(2)313-322(1980) 2.Brin, M.The antithiamine effects of amprolium in rats on tissue transketolase activityToxicol. Appl. Pharmacol.6(4)454-458(1964) 3.Joyner, L.P., and Norton, C.C.The anticoccidial effects of amprolium, dinitolmide and monensin against Eimeria maxima, E. brunetti and E. acervulina with particular reference to oocyst sporulationParasitology75(2)155-164(1977) 4.Abbas, R.I., Manzoor, Z., Munawar, S.H., et al.Anticoccidial activity of hydrochloric acid (HCl) against Eimeria tenella in broiler chickensPesq. Vet. Bras.31(5)425-429(2011) 5.Chornyy, S., Parkhomenko, J., and Chorna, N.Thiamine deficiency caused by thiamine antagonists triggers upregulation of apoptosis inducing factor gene expression and leads to caspase 3-mediated apoptosis in neuronally differentiated rat PC-12 cellsActa. Biochim. Pol.54(2)315-322(2007)
| Cas No. | 121-25-5 | SDF | |
| 别名 | 氨丙啉 | ||
| Canonical SMILES | CC1=CC=CC=[N+]1CC2=CN=C(CCC)N=C2N.[Cl-] | ||
| 分子式 | C14H19ClN4 | 分子量 | 278.78 |
| 溶解度 | Soluble in DMSO | 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 | 3.5871 mL | 17.9353 mL | 35.8706 mL |
| 5 mM | 0.7174 mL | 3.5871 mL | 7.1741 mL |
| 10 mM | 0.3587 mL | 1.7935 mL | 3.5871 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 | ||||||||||
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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。
Amprolium exposure alters mice behavior and metabolism in vivo
Animal Model Exp Med 2018 Nov 21;1(4):272-281.PMID:30891577DOI:10.1002/ame2.12040.
Background: Thiamine deficiency (TD) models have been developed, mainly using the thiamine analog pyrithiamine. Other analogs have not been used in rodents. We aimed to evaluate the effects and mechanisms of intraperitoneal (ip) amprolium-induced TD in mice. We also evaluated the associated pathogenesis using antioxidant and anti-inflammatory compounds (Trolox, dimethyl sulfoxide). Methods: Male mice were separated into two groups, one receiving a standard diet (control animals), and the other a TD diet (deficient groups) for 20 days. Control mice were further subdivided into three groups receiving daily ip injections of saline (NaCl 0.9%; Cont group), Tolox (Tr group) or dimethyl sulfoxide (DMSO; Dmso group). The three TD groups received Amprolium (Amp group), Amprolium and Trolox (Amp+Tr group), or Amprolium and DMSO (Amp+Dmso group). The animals were subjected to behavioral tests and then euthanized. The brain and viscera were analyzed. Results: Amprolium exposure induced weight loss with hyporexia, reduced the behavioral parameters (locomotion, exploratory activity, and motor coordination), and induced changes in the brain (lower cortical cell viability) and liver (steatosis). Trolox co-treatment partially improved these conditions, but to a lesser extent than DMSO. Conclusions: Amprolium-induced TD may be an interesting model, allowing the deficiency to develop more slowly and to a lesser extent. Amprolium exposure also seems to involve oxidative stress and inflammation, suggested as the main mechanisms of cell dysfunction in TD.
Evaluation of sulfadimidine, Amprolium and triquen to treat coccidiosis in wild pigeons
Braz J Biol 2021 Mar 12;82:e238673.PMID:33729384DOI:10.1590/1519-6984.238673.
Coccidiosis remains one of the major problems in poultry all over the world. Very limited data on anticoccidial drugs in wild pigeons is available. The current study was aimed to understand the comparative efficacy of sulfadimidine, Amprolium and triquen in wild pigeons of Dir district, Pakistan suffering from coccidiosis. The faecal matter of wild pigeons were purchased from the local market for coccidian infection. Results revealed that 88.8% (16/18) were found infected with Eimeria spp. Three positive groups were treated with sulfadimidine (0.2mg/L), Amprolium (25mg/L) and triquen. Sulfadimidine was most effective (45%) followed by Amprolium (44.6%) while triquen (24.0%) showed less effectiveness against coccidiosis in pigeons. Number of oocysts were 79, 81 and 80 before treatment and 60, 44 and 44 after treatment with sulfadimidine, Amprolium and triquen respectively. This study showed that sulphadimidine, Amprolium and triquen could not significantly reduce the coccidiosis in pigeons. Further studies are required to clear the mechanism of anti-coccidial drugs in wild pigeons.
Supplemental use of liquid Amprolium in skip-a-day feeding of replacement pullets
Poult Sci 1991 Mar;70(3):515-20.PMID:2047345DOI:10.3382/ps.0700515.
The addition of liquid Amprolium to the drinking water on days when medicated (Amprolium) ration was not fed in a restricted feeding (skip-a-day) program improved protection against a primary exposure to Eimeria acervulina and Eimeria tenella, yet still allowed for the development of protective immunity to subsequent challenge. With E. tenella, the best protection, as measured by reduction of lesion score, was provided by Amprolium given in the drinking water on alternate days to feed medication when compared with the use of Amprolium only in the feed or liquid Amprolium at less frequent intervals (every second or third nonfeeding day). With Eimeria maxima, Amprolium in the feed did not significantly lower lesion score compared with the score in unmedicated pullets; however, the further addition of Amprolium to the drinking water did. When pullets were reared in floor pens previously seeded with coccidia, Amprolium medication in the feed alone reduced the E. tenella-induced mortality rate from 28 to 8%. The addition of Amprolium in the drinking water on nonfeeding days eliminated all deaths. Floor-reared pullets were caged after 3 wk and challenged 1 wk later with the same species of coccidial oocysts used to immunize on the floor. Coccidial lesion scores following challenge were eliminated or markedly lower than in pen-reared (unimmunized) pullets similarly challenged. This indicated that protective immunity developed despite the use of Amprolium in the drinking water.
Effect of Amprolium on production, sporulation, and infectivity of Eimeria oocysts
Avian Dis 1993 Oct-Dec;37(4):988-92.PMID:8141759doi
Amprolium reduced the number of oocysts shed by Eimeria acervulina, E. maxima, E. necatrix, and a mixture of susceptible strains of E. tenella. Sporulation of oocysts from mediated chickens was reduced compared with that of oocysts from unmedicated chickens. Sporulation was reduced by levels of 0.0250% Amprolium for E. acervulina and by levels of 0.0060% for E. maxima and the susceptible E. tenella. Not enough oocysts were recovered to measure sporulation of E. necatrix. Sporulation reduction was not affected by the method of administration of Amprolium (feed or water), except with E. acervulina, for which fewer oocysts sporulated when 0.0120% Amprolium was added in the drinking water than when 0.0125% Amprolium was added to the feed. Conversely, Amprolium medication had no effect on the sporulation of an amprolium-resistant E. tenella. When fed to unmedicated chickens, those oocysts from amprolium-medicated chickens that did sporulate were as infective as oocysts recovered from unmedicated chickens.
Kinetic behaviour of sulphaquinoxaline and Amprolium in chickens
Dtsch Tierarztl Wochenschr 1995 Dec;102(12):481-5.PMID:8591749doi
The pharmacokinetics of sulphaquinoxaline and Amprolium hydrochloride were studied in Hubbard broiler chickens. Single doses of sulphaquinoxaline (100 mg/kg b. wt.), and Amprolium hydrochloride (30 mg/kg b. wt.) were administered orally and intravenously to the same birds with 15 days interval between treatments. Sulphaquinoxaline and Amprolium HCl were determined colorimetrically. Following i.v. administration, the concentration-time curve of sulphaquinoxaline and Amprolium could be explained by a two compartments open model with a t1/2 alpha of 0.16 +/- 0.008 h; 0.17 +/- 0.09 h; t1/2 beta of 12.6 +/- 0.32 h, 4.89 +/- 0.3 h respectively. The total body clearance were 0.278 +/- 0.013 ml/kg/min; 0.562 +/- 0.015 ml/kg/min; volume of distribution at steady state were 0.44 +/- 0.009 L/kg, 0.34 +/- 0.005 L/kg and systemic bioavailability following oral administration were 72.65 +/- 3.38, 66.09 +/- 4.9 percent for sulphaquinoxaline and Amprolium HCl respectively. Following oral administration of sulphaquinoxaline and Amprolium (the same previous doses) the peak plasma concentrations (Cmax) were 107.8 +/- 1.49 micrograms/ml; 42.9 +/- 1.11 micrograms/ml and occurred at 5.56 +/- 0.1 h, 3.67 +/- 0.05 h respectively. Pharmacokinetic parameters after repeated oral daily administrations of sulphaquinoxaline and Amprolium revealed that the Cmax was 184 +/- 1.02 micrograms/ml, and 55.19 +/- 0.35 micrograms/ml at 7.36 +/- 0.18 h and 5.17 +/- 0.15 h and the biological half lives were 1.67 +/- 0.057 h and 1.11 +/- 0.14 h respectively. Sulphaquinoxaline and its N4 acetyl metabolite disappeared from all body tissues at 120 hours, however Amprolium persisted in most tissues for 72 hours after the last dose of repeated administrations.