β-lactam
Penicillin G binds to TEM-1 β-lactamase with a binding constant (Ka) of 1.41×10⁷ L/mol at 278 K, indicating strong affinity through hydrogen bonding and Van der Waals forces. The binding is spontaneous and exothermic.[1]

青霉素G钠盐-TEM-1系统的紫外-可见(UV-Vis)吸收光谱与青霉素G钠盐和TEM-1 β-内酰胺酶的吸收光谱显着不同，表明两种酶之间形成了新的复合物。随着青霉素G钠盐浓度的增加，TEM-1β-内酰胺酶的紫外-可见吸收增加，并出现轻微的红移，表明青霉素G钠盐与TEM-1β-内酰胺酶之间的相互作用引起轻微的红移。 TEM-1 β-内酰胺酶的构象变化[1]。

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Penicillin G 与 TEM-1 β-内酰胺酶相互作用，导致酶的静态荧光猝灭和构象变化。结合由焓变驱动，结合常数随温度升高而降低（278 K 时为 1.41×10⁷ L/mol，288 K 时为 7.62×10⁶ L/mol）。结合位点数约为 1，表明形成 1:1 复合物。TEM-1 与青霉素 G 之间的能量转移距离为 2.08 nm。[1]

根据logistic回归模型，青霉素G钠盐处理组的猪拭子阳性概率比对照组低1.6倍（P<0.05）。与每板零菌落相比，对照组拭子含有10至99个菌落的风险是接受青霉素G钠盐处理的猪的2.3倍（P=0.022）[2]。

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在一项涉及896头断奶仔猪（18日龄）的田间试验中，通过饮用水给予Potassium Penicillin G（剂量为每升水297,000 IU），进行两个为期5天的治疗期（断奶后第1-5天和第21-25天），显著降低了死亡率和猪链球菌携带率。治疗组的总死亡率为7.1%（32/448头猪），而对照组为14.0%（59/420头猪）。治疗组中归因于猪链球菌的死亡率（29头猪）也显著低于对照组（53头猪）。与对照组相比，治疗组猪的扁桃体猪链球菌携带量（每板≥1000菌落）也显著降低。[2]

将 TEM-1β-内酰胺酶溶液 (5×10-6 M) 与不同浓度的头孢氨苄、头孢西丁和青霉素 G 钠盐溶液在 278 K 下混合。将三种抗生素逐渐添加至浓度 0 至 25×10 -6 M. 混合和相互作用 2 分钟后，用 2 nm 狭缝和 400 nm/min 扫描速度的分光光度计记录紫外-可见 (UV-Vis) 吸收光谱，并加入 0.02 M 磷酸盐缓冲液 (pH 7.0)作为参考[1]。

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在 278 K 下，于磷酸缓冲液（pH 7.0）中，记录 TEM-1 β-内酰胺酶（5.0×10⁻⁶ mol/L）与不同浓度 penicillin G（0–25×10⁻⁶ mol/L）的紫外-可见吸收光谱。光谱显示增色效应和红移，表明复合物形成。[1]
在 278 K、283 K 和 288 K 下，于激发波长 278 nm 和 295 nm 处，测量 TEM-1 β-内酰胺酶（2.5×10⁻⁷ mol/L）与不同浓度 penicillin G（0–11.25×10⁻⁸ mol/L）的荧光发射光谱。使用 Stern-Volmer 方程和修正的 Stern-Volmer 方程分析猝灭数据，以确定猝灭常数和结合参数。[1]
记录同步荧光光谱（Δλ = 15 nm 用于酪氨酸，Δλ = 60 nm 用于色氨酸）以监测结合后的构象变化。[1]
进行碘化钾猝灭实验，以评估 TEM-1 和 TEM-1-penicillin G 复合物中发色团残基的表面可及性。[1]

For this study, a randomized complete block design with two replicates is employed. With 16 pens and 28 pigs per pen, a replicate has 448 pigs total. Pigs are also sorted by weight, with animals grouped together in blocks according to visual observation of similar weight. Through the use of a formal randomization procedure, two treatments are assigned at random within each block of two adjacent pens. The two treatment groups are Treated (sodium salt of penicillin G) and Control (no treatment). Drinking water containing Penicillin G sodium salt is given for five days during two treatment sessions. Day 1 (the day the pigs are moved into the nursery barns) marks the start of the first treatment period, which ends on Day 5. Day 21 marks the start of the second treatment phase, which lasts until Day 25. There is no treatment given to the Control group[2].

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A total of 896 eighteen-day-old weaned pigs from a commercial farm with a history of S. suis serotype 2 infection were used. Pigs were blocked by sex and weight and randomly assigned to either a treatment group or a control group within pens. The treatment group received Potassium Penicillin G in drinking water at a final calculated dose of 297,000 IU per liter. The drug was prepared by dissolving 85-gram aliquots in water to create a stock solution, which was then delivered via a proportioner into the watering system at a ratio of 1:128 (stock:water). Fresh stock solution was prepared twice daily. Treatment was administered for 5 days during two separate periods: starting on the day of weaning (Day 1) and again on Day 21 post-weaning. The control group received no treatment. Tonsillar swabs were collected from four randomly selected pigs per pen at three time points: Day 1 (pre-treatment), Day 6 (post-first treatment), and Day 26 (post-second treatment) for bacterial culture and quantification.[2]
Pigs showing clinical signs of S. suis infection (ataxia, tremors, lateral recumbency) were treated individually with an intramuscular injection of ceftiofur hydrochloride (3 mg/kg). If more than three pigs in a pen showed signs, the entire pen was treated. Seriously ill or moribund pigs were euthanized and submitted for necropsy to confirm cause of death.[2]

[1]. Spectroscopic analysis and docking simulation on the recognition and binding of TEM-1 β-lactamase with β-lactam antibiotics. Exp Ther Med. 2017 Oct;14(4):3288-3298.

[2]. Decreased mortality of weaned pigs with Streptococcus suis with the use of in-water potassium penicillin G. Can Vet J. 2011 Mar;52(3):272-6.

Sodium penicillin G is a white to slightly yellow crystalline powder with a slight odor. The pH (10% solution) is 5.5–7.5. (NTP, 1992)
Sodium benzylpenicillin is an organosodium salt. It contains a benzylpenicillin (1-) group.
Penicillin G (potassium or sodium) is a prescription antimicrobial drug approved by the U.S. Food and Drug Administration (FDA) for the treatment of certain serious bacterial infections, such as pneumonia, meningitis, gonorrhea, and syphilis.
Pneumonia and syphilis may be opportunistic infections associated with HIV.
Sodium penicillin G is the sodium salt form of benzylpenicillin, a semi-synthetic broad-spectrum penicillin antibiotic with bactericidal activity. Sodium benzylpenicillin binds to and inactivates penicillin-binding protein (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBP interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of the bacterial cell wall. This leads to weakening of the bacterial cell wall, ultimately resulting in cell lysis.
Benzylpenicillin sodium is a penicillin derivative that is usually used in sodium or potassium form to treat a variety of infections. It is effective against most Gram-positive and Gram-negative cocci. It has also been used as an experimental convulsant due to its action on γ-aminobutyric acid (GABA)-mediated synaptic transmission.
See also: Penicillin G (with active moiety).

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Penicillin G is a β-lactam antibiotic whose structure contains a β-lactam ring fused with a thiazolidinyl ring. It binds to TEM-1 β-lactamase mainly by forming hydrogen bonds with residues Ala237, Ser70, Ser130, Asn132, Arg244, and Ser235, forming a total of 6 hydrogen bonds. This binding induces a conformational change in the enzyme, increasing the polarity around the tryptophan residues. This study provides insights into the design of novel antibiotics against TEM-1 β-lactamase. [1]

C16H17N2NAO4S

356.3720

356.08

C, 53.93; H, 4.81; N, 7.86; Na, 6.45; O, 17.96; S, 9.00

69-57-8

Penicillin G potassium;113-98-4;Penicillin G procaine hydrate;6130-64-9;Penicillin G benzathine;1538-09-6;Penicillin G benzathine tetrahydrate;41372-02-5;Penicillin G;61-33-6

23668834

White to off-white solid powder

1.41

663.3ºC at 760 mmHg

209-212°C

300 ° (C=2, H2O)

114.84

1

5

4

24

536

3

S1C(C([H])([H])[H])(C([H])([H])[H])[C@]([H])(C(=O)[O-])N2C([C@]([H])([C@@]12[H])N([H])C(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)=O.[Na+]

FCPVYOBCFFNJFS-LQDWTQKMSA-M

InChI=1S/C16H18N2O4S.Na/c1-16(2)12(15(21)22)18-13(20)11(14(18)23-16)17-10(19)8-9-6-4-3-5-7-9;/h3-7,11-12,14H,8H2,1-2H3,(H,17,19)(H,21,22);/q;+1/p-1/t11-,12+,14-;/m1./s1

4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 3,3-dimethyl-7-oxo-6-((2-phenylacetyl)amino)- (2S,5R,6R)-, sodium salt (1:1)

Benzylpenicillin sodium salt; Penicillin G sodium salt; Monosodium benzylpenicillin; Mycofarm; Novocillin; NSC 402815; OK 431; Pen-A-Brasive;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： (1). 该产品在溶液状态不稳定，请现配现用。  (2). 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

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

DMSO : 71~100 mg/mL ( 199.23~280.61 mM )
Water : 71~125 mg/mL(~350.76 mM)
Ethanol : ~1 mg/mL

配方 1 中的溶解度: ≥ 2.5 mg/mL (7.02 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (7.02 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (7.02 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (7.02 mM)

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配方 5 中的溶解度: 100 mg/mL (280.61 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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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。