Bacterial cell wall synthesis; β-lactam

Ampicillin tri水合物（D-(-)-α-氨基苄青霉素三水合物）以剂量依赖性方式抑制猪源大肠杆菌的生长。三水氨苄青霉素的有效抑菌浓度为2.5 uG/mL[1]。

三水氨苄青霉素（D-(-)-α-氨基苄青霉素三水合物）对于缓解11周龄猪出血性肠炎的症状非常有效[1]。氨苄西林三水合物在胆汁中的最大浓度是血清中的两倍。氨苄青霉素口服后在门静脉血中的峰值浓度是外周血中的两倍[2]。氨苄西林三水合物可提供针对缺血再灌注脑损伤的神经保护作用。 Ampicillin tri Hydro 可降低 MMP 的活性并增加 GLT-1 的表达水平。三水氨苄青霉素预处理可显着减少整体前脑缺血后的内侧海马细胞死亡[3]。

敏感性测试[1]
在每一种浓度的抗生素下，一组5个重复管分别接种1滴，每滴1滴的试验培养物生长18小时。接种管37℃孵育。6小时后，用0.5%终浓度的福尔马林停止进一步生长。用带有525 μ m滤光片的Fisher电光度计记录培养物的生长和光密度。

研究了从精练猪和非精练猪分离的103个大肠杆菌培养物和从一例坏死性肠炎分离的4个沙门氏菌培养物对氨苄西林的体外敏感性，这些氨苄西林的浓度分别为0、0.1、1.0和5.0 uG / ml。除3株外，其余培养的大肠杆菌均对5.0 uG/ml敏感。在美国，所有分离的沙门氏菌也对该浓度的抗生素敏感。大肠杆菌的敏感性也通过用含有0、0.1、1.0、2.5、5.0和10.0 uG / ml氨苄西林的E.M.B.琼脂培养液镀取精练猪或非精练猪的粪便样品进行测试。在0、0.1和1.0 uG浓度下，大肠杆菌的生长没有差异。三种较高浓度的抗生素对大肠杆菌生长的抑制作用与氨苄青霉素在每种浓度中的含量成正比。 氨苄西林被证明对减轻11周龄猪出血性肠炎的症状非常有效。scours的消失与先前存在的粪便大肠杆菌的血清生物型被另一种产生H2S的异常型大肠杆菌所取代有关。在用这种抗生素治疗动物后，没有出现耐氨苄西林的大肠杆菌菌株。[1]

Ampicillin (200 mg/kg/day) and penicillin G sodium salt (6,000 U/kg or 20,000 U/kg) were dissolved in normal saline and administered intraperitoneally (i.p.) for 5 days. Forebrain ischemia was induced as described earlier 24 h after the last injection. To elucidate the molecular mechanism of ampicillin, dihydrokainic acid (DHK) (10 mg/kg), a GLT-1 inhibitor, was administrated i.p. 30 min before the onset of ischemia. In the control animals, saline was administered instead of ampicillin or penicillin G, at the same volume and time schedule.[3]

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Ampicillin was tested on a 11-week old pig suffering from hemorrhagic enteritis. The antibiotic was administered orally in gelatin capsules. An initial dose of 8 mg/ Kg body weight was followed by two, 4 mg/Kg doses at 4 hour intervals. Fecal samples were obtained from the above scouring pig before the administration of the antibiotic and 48 hours after the first dose, by that time the animal had recovered. A third fecal sample was obtained from a healthy pig in another litter as a control. Dilutions of 'the fecal samples ranging up to 10-8 were plated in E.M.B. agar medium containing 0, 0.1, 1.0, 2.5, 5.0 and 10.0 uG of Ampicillin per ml. of the medium. The plates were incubated at 37°C. for 48 hours and the typical E. coli were enumerated. Seven representative colonies of E. colti were isolated from each fecal sample and characterized biochemically following Kaufmann's (5) scheme. The cultures were also identified serologically by employing 0 and K antisera prepared against six well described E. coli serotypes (E145, E681, E68II, G7, E4 and E57), isolated from diseased swine (Sojka, 10, 11). Antibiotic sensitivity of all the isolates was tested by employing sensi-discs4 of chlortetracycline, oxytetracycline, 30 and 5 uG each, Bacitracin, penicillin, 10 I.U. each, and Ampicillin5, 10 uG. A few E. coli colonies which grew in E.M.B. media containing 5.0 and 10.0 uG of Ampicillin per ml. were tested for their susceptibility to 10.0 uG Ampicillin with sensitivity discs.[1]

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Substantial information indicates that ampicillin produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with penicillins, but these effects have not been adequately evaluated. Ampicillin is acceptable in nursing mothers.
◉ Effects in Breastfed Infants
An uncontrolled observation of the breastfed infants of mothers taking ampicillin noted a seeming increase in cases of diarrhea and candidiasis that was attributed to ampicillin in breastmilk.
In a prospective follow-up study, 5 nursing mothers reported taking ampicillin (dosage unspecified). One mother reported diarrhea in her infant. No rashes or candidiasis were reported among the exposed infants.
A small, controlled, prospective study had mothers monitor their infants for signs of adverse effects (furring of the tongue, feeding difficulties, changes in stool frequency and consistency, diaper rash, and skin rash). Weight change and the development of jaundice were also recorded. No statistical differences in these parameters were found between the infants of the control mothers and those of mothers taking ampicillin.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[1]. Effect of Ampicillin on E. Coli of Swine Origin. Can J Comp Med Vet Sci. 1963 Sep;27(9):223-7.

[2]. Ampicillin in portal and peripheral blood and bile after oral administration of ampicillin andpivampicillin. Eur J Clin Pharmacol. 1974;7(2):133-5.

[3]. The neuroprotective mechanism of ampicillin in a mouse model of transient forebrain ischemia. Korean J Physiol Pharmacol. 2016 Mar;20(2):185-92.

Ampicillin trihydrate is an odorless white microcrystalline powder with a bitter taste. A 0.25% solution in water has a pH of 3.5 to 5.5. (NTP, 1992)
Ampicillin trihydrate is a hydrate. It contains an ampicillin.
Ampicillin Trihydrate is the trihydrate form of ampicillin, a broad-spectrum semisynthetic derivative of aminopenicillin. Ampicillin trihydrate inhibits bacterial cell wall synthesis by binding to penicillin binding proteins, thereby inhibiting peptidoglycan synthesis, a critical component of the bacterial cell wall.
Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.

C16H25N3O7S

403.45

403.141

C, 47.63; H, 6.25; N, 10.42; O, 27.76; S, 7.95

7177-48-2

Ampicillin;69-53-4;Ampicillin sodium;69-52-3; 69-53-4 (free acid); 23277-71-6 (potassium); 114977-84-3 (trimer trisodium) ; 69-52-3 (sodium); 7490-86-0 (hemisulfate); 33276-75-4 (benzathine); 119229-01-5 (embonate); 40688-84-4 (HCl); 7177-48-2 (trihydrate);

23565

White to light yellow solid powder.

683.9ºC at 760 mmHg

208 °C (dec.)(lit.)

367.4ºC

265 ° (C=0.1, H2O)

1.154

165.72

6

9

4

27

562

4

S1C(C([H])([H])[H])(C([H])([H])[H])[C@]([H])(C(=O)O[H])N2C([C@]([H])([C@@]12[H])N([H])C([C@@]([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])[H])=O)=O

RXDALBZNGVATNY-CWLIKTDRSA-N

InChI=1S/C16H19N3O4S.3H2O/c1-16(2)11(15(22)23)19-13(21)10(14(19)24-16)18-12(20)9(17)8-6-4-3-5-7-8/h3-7,9-11,14H,17H2,1-2H3,(H,18,20)(H,22,23)3*1H2/t9-,10-,11+,14-/m1.../s1

(2S,5R,6R)-6-((R)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate

Amcill; Aminobenzyl Penicillin; KS-R1; KS R1; KSR1; Omnipen; Pentrexyl; 615-347-9; 7177-48-2; Ampicillin trihydrate; Aminobenzylpenicillin trihydrate; Principen; Penbritin; AMPICILLIN/AMPICILLIN TRIHYDRATE; HXQ6A1N7R6; Polycillin; Ukapen

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~81 mg/mL ( ~200.76 mM )
Water : 2~4.55 mg/mL(~11.28 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。