Penicillin-binding proteins (PBPs) [1,2]
β-lactam

- 厌氧菌活性：厄他培南对99.1%的临床重要厌氧菌具有活性，对脆弱拟杆菌和普通拟杆菌的MIC90值≤1 μg/mL，众数MIC为0.12 μg/mL [1]
- 革兰阴性菌覆盖：对产超广谱β-内酰胺酶（ESBLs）或AmpC酶的肠杆菌科细菌有效，对大肠杆菌和肺炎克雷伯菌的MIC90值≤2 μg/mL [1]
在大约48小时内，厄他培南二钠（0-100 μg/mL）可以有效对抗99.1%的厌氧菌，其模式MIC为0.12 μg/mL，MIC90为1 μg/mL，MIC≥8 μg/mL。分别针对 B. fragilis 和 B. vulgatus 物种[1]。

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针对367株临床厌氧菌分离株，Ertapenem 表现出强效活性：对脆弱拟杆菌（Bacteroides fragilis）的MIC₉₀为0.5 μg/mL，普雷沃菌属（Prevotella spp.）为0.25 μg/mL，梭杆菌属（Fusobacterium spp.）为0.12 μg/mL，产气荚膜梭菌（Clostridium perfringens）为0.25 μg/mL。其对产β-内酰胺酶脆弱拟杆菌的活性优于头孢替坦和哌拉西林-他唑巴坦。[1] Ertapenem 对产超广谱β-内酰胺酶（ESBL）肠杆菌保持活性，90%菌株的MIC ≤0.5 μg/mL。[2]

- 长效特性：在小鼠大腿感染模型中，皮下注射10 mg/kg厄他培南的血浆半衰期为1.3小时，对金黄色葡萄球菌的杀菌效果维持>3 log10 CFU减少 [2]
- 复杂感染疗效：在大鼠腹腔脓毒症模型中，厄他培南（50 mg/kg静脉注射）与亚胺培南/西司他丁疗效相当，细菌清除率超过90% [2]
在小鼠大腿感染模型中，Ertapenem（单次皮下给药25 mg/kg）24小时内使大肠杆菌和肺炎克雷伯菌载菌量降低3.5–4.0 log₁₀ CFU/大腿，疗效与血药浓度高于MIC的时间（T > MIC）超过35%相关。[2]
使用金黄色葡萄球菌大腿组织感染模型，厄他培南二钠（皮下注射，0-10 mg/kg，感染后 0-120 小时）在 10 mg/kg 时使微生物减少 > 3 log10 CFU，并将活性保持在 3.3 和4.4 log10 CFU 以 2 mg/kg 去除[2]。除了对所有革兰氏阳性菌有效外，厄他培南二钠（皮下注射，感染后 4 小时，全身感染模型）也对革兰氏阴性菌有效，ED50 小于 0.25 mg/kg/剂[2]。

PBPs结合实验： 1. 含PBPs的膜组分（0.5 mg/mL）与厄他培南（0.01–10 μM）在Tris-HCl缓冲液（pH 7.5）中37°C孵育20分钟。 2. 通过放射性标记的[³H]苄青霉素置换法检测结合，随后进行SDS-PAGE和放射自显影。 3. 厄他培南对PBP-2和PBP-3的IC50分别为0.08 μM和0.15 μM [2]

细胞活力测定[1]
细胞类型： fragilis (ATCC 25285)、B. thetaiotaomicron (ATCC 29741) 和 lentum (ATCC 43055)
测试浓度： 大约 0-100 μg/ mL
孵育时间： 48 小时
实验结果： 使用 MIC 模式抑制所有分离株的 99.1% 0.12 μg/mL，MIC90 1 μg/mL，脆弱拟杆菌组中 98.8% 的分离株易感。

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细菌生长抑制实验： 1. 脆弱拟杆菌（10⁶ CFU/mL）在布鲁氏菌肉汤中暴露于厄他培南（0.06–256 mg/L）。 2. 37°C孵育48小时后测定MIC终点。 3. 厄他培南对90%菌株的MIC≤1 mg/L [1]

Animal/Disease Models: S. aureus thigh tissue infection model (DBA/2 mice)[2]
Doses: 0.5,1, 2, 5, 10 mg/kg (given at 2, 6, 10 , 24, 48, 72, 96, 120 h)
Route of Administration: subcutaneous (sc) injection (0.5 mL after infection)
Experimental Results: Displayed > 3 log10 CFU reduction of organism compared to non-antibiotic-treated controls at 10 mg/kg. Maintained the activity with 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg.

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Animal/Disease Models: Systemic infection model (DBA/2 female mice, viral antibody-free CD-1 female mice)[2]
Doses: 0-3 mg/kg approximately
Route of Administration: subcutaneous (sc) injection (0.5 mL, begin immediately and 4 h after infection)
Experimental Results: demonstrated activity against all gram-positive organisms, and also ram-negative organisms tested with ED50s of <0.25 mg/kg/dose.

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Animal/Disease Models: CD-1 mice, rats[2]
Doses: 10 mg/kg approximately
Route of Administration: intraperitoneal (ip)injection (pharmacokinetic/PK assay)
Experimental Results: demonstrated an AUC0-∞ ranging from 1.8-21.82 μg·hr/mL in tissue in mice following a 10-mg/kg ip dose. demonstrated slow

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Murine Thigh Infection Model: Mice were inoculated intramuscularly with 10⁶ CFU of E. coli or K. pneumoniae. Ertapenem was dissolved in 10% sodium bicarbonate solution and administered subcutaneously at 25 mg/kg as a single dose 2 hours post-infection. Bacterial loads were quantified 24 hours post-treatment. [2]
Rat Pharmacokinetics Study: Rats received Ertapenem intravenously (20 mg/kg) or subcutaneously (40 mg/kg). Blood samples were collected serially over 24 hours for PK analysis. [2]

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- Murine Peritonitis Model: 1. ICR mice were infected intraperitoneally with E. coli (10⁹ CFU). 2. Ertapenem (10–100 mg/kg) was administered subcutaneously every 12 hours for 3 days. 3. Survival rates were monitored for 7 days, with 100% survival at doses ≥50 mg/kg [2]

- Plasma Half-life: 1.3 hours in mice after subcutaneous administration; 4 hours in humans [2]
- Renal Excretion: Approximately 80% of the dose was excreted in urine, with 38% as unchanged drug and 37% as metabolites [2]
- Protein Binding: 95% plasma protein binding in humans [2]

- Central Nervous System Effects: In preclinical studies, ertapenem caused seizures in rats at doses ≥200 mg/kg, likely due to competitive binding to GABA receptors [2]
- Renal Safety: No significant nephrotoxicity was observed in animal studies at therapeutic doses [2]

[1]. Kenneth E Aldridge. Ertapenem (MK-0826), a new carbapenem: comparative in vitro activity against clinically significant anaerobes. Diagn Microbiol Infect Dis. 2002 Oct;44(2):181-6.

[2]. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, MK-826 (L-749,345). Antimicrob Agents Chemother. 1998 Aug;42(8):1996-2001.

- Mechanism of Action: Ertapenem irreversibly inhibits PBPs, disrupting peptidoglycan cross-linking and causing bacterial cell lysis [1,2]
- Clinical Indications: Approved for treating complicated intra-abdominal infections, skin/skin structure infections, and community-acquired pneumonia caused by susceptible pathogens [1,2]
- Limitations: Not active against Pseudomonas aeruginosa or Enterococcus faecium [1,2]

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Ertapenem Sodium is the sodium salt of ertapenem, a 1-beta-methyl carbapenem and a broad-spectrum beta-lactam antibiotic with bactericidal activity. Ertapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, in particular PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. Inhibition of peptidoglycan synthesis results in weakening and lysis of the cell wall and cell death. In vitro, this agent has shown activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Erapenem is resistant to hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases.
A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.
See also: Ertapenem Sodium (annotation moved to).

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Drug Indication
TreatmentErtapenem SUN is indicated in paediatric patients (3 months to 17 years of age) and in adults for the treatment of the following infections when caused by bacteria known or very likely to be susceptible to ertapenem and when parenteral therapy is required (see sections 4. 4 and 5. 1): - Intra-abdominal infections- Community acquired pneumonia- Acute gynaecological infections- Diabetic foot infections of the skin and soft tissue (see section 4. 4)PreventionErtapenem SUN is indicated in adults for the prophylaxis of surgical site infection following elective colorectal surgery (see section 4. 4). Consideration should be given to official guidance on the appropriate use of antibacterial agents.
TreatmentTreatment of the following infections when caused by bacteria known or very likely to be susceptible to ertapenem and when parenteral therapy is required: intra-abdominal infections; community-acquired pneumonia; acute gynaecological infections; diabetic foot infections of the skin and soft tissue. PreventionInvanz is indicated in adults for the prophylaxis of surgical site infection following elective colorectal surgery. Consideration should be given to official guidance on the appropriate use of antibacterial agents.

C22H23N3NA2O7S

519.48

497.123

153832-38-3

Ertapenem sodium;153773-82-1;Ertapenem;153832-46-3;Ertapenem-d4 disodium;1356934-56-9

150611

White to off-white solid powder

813.9ºC at 760 mmHg

230-234ºC (dec.)

446ºC

5.26E-28mmHg at 25°C

0.394

190.72

3

9

5

35

882

6

C[C@@H]1[C@@H]2[C@H](C(=O)N2C(=C1S[C@H]3C[C@H](NC3)C(=O)NC4=CC=CC(=C4)C(=O)[O-])C(=O)[O-])[C@@H](C)O.[Na+].[Na+]

KMVRATCHVMUJHM-SHZCTIMHSA-L

InChI=1S/C22H25N3O7S.2Na/c1-9-16-15(10(2)26)20(28)25(16)17(22(31)32)18(9)33-13-7-14(23-8-13)19(27)24-12-5-3-4-11(6-12)21(29)30;;/h3-6,9-10,13-16,23,26H,7-8H2,1-2H3,(H,24,27)(H,29,30)(H,31,32);;/q;2*+1/p-2/t9-,10-,13+,14+,15-,16-;;/m1../s1

disodium;(4R,5S,6S)-3-[(3S,5S)-5-[(3-carboxylatophenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate

Ertapenem disodium; 153832-38-3; Ertapenem sodium; Ertapenem Disodium 90%; P5HEA33D9R; disodium;(4R,5S,6S)-3-[(3S,5S)-5-[(3-carboxylatophenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate; 153773-82-1; UNII-P5HEA33D9R;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

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。