用美洛西林进行体内治疗（皮下注射；1.7–5.7 mg/kg；每天两次；7天）可抑制迟发型超敏反应、IgM和IgG反应、脱发以及淋巴细胞增殖剂量减少[1]。

Animal/Disease Models: Male balb/c (Bagg ALBino) mouse [1]
Doses: 1.7, 4.3, and 5.7 mg/kg
Route of Administration: subcutaneous injection; 1.7, 4.3, and 5.7 mg/kg; twice (two times) daily; 7-day
Experimental Results: All dose treatments were Inhibits IgM and IgG responses as well as delayed-type hypersensitivity reactions. Hair loss was observed in most animals treated at all doses. Inhibits lymphocyte proliferation in animal spleen cell cultures.

Metabolism / Metabolites
Unlike many other penicillin-type drugs, Mezlocillin is either extensively metabolized or primarily excreted via bile, as only about 50% of the dose is detected in normal urine. Biological Half-Life 1.3 to 4.4 hours

Protein Binding
16-59%

[1]. Antibiotics and immunomodulation: effects of cefotaxime, amikacin, mezlocillin, piperacillin and clindamycin. Med Microbiol Immunol. 1985;173(5):279-89.

[2]. Mezlocillin: in vitro studies of a new broad-spectrum penicillin. Antimicrob Agents Chemother. 1977 Jan;11(1):74-9.

[3]. Treatment of accidental high dose intraventricular mezlocillin application by cerebrospinal fluid exchange. J Neurol Neurosurg Psychiatry. 1998 Mar;64(3):379-81.

Mezlocillin is a penicillin with a (2R)-2-[3-(methanesulfonyl)-2-oxoimidazolidine-1-carbamoyl]-2-phenylacetamyl group at the 6-position of its penicillin ring. It is an antibacterial drug. It is both a penicillin and a penicillin allergen. It is the conjugate acid of Mezlocillin (1-). It is a semi-synthetic ampicillin-derived acylurea penicillin. It has been proposed for the treatment of certain anaerobic bacterial infections and may be effective against inner ear, bile, and central nervous system infections. Mezlocillin has been reported in cattle and honeybees, with relevant data. Mezlocillin is a broad-spectrum β-lactam penicillin antibiotic with antibacterial activity. Mezlocillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls. Inactivation of PBPs interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of bacterial cell walls. This interrupts the final stage of bacterial cell wall synthesis, leading to weakened bacterial cell walls and ultimately cell lysis.
A semi-synthetic ampicillin-derived acylurea penicillin. It has been proposed for the treatment of certain anaerobic bacterial infections and may be effective against inner ear, biliary tract, and central nervous system infections.
See also: Mezlocillin sodium (note moved to).

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Drug Indications
For the treatment of severe infections of the lungs, urinary tract, and skin caused by Gram-negative bacteria.

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Mechanism of Action
Mezlocillin inhibits the third (and final) stage of bacterial cell wall synthesis by binding to a specific penicillin-binding protein (PBP) located within the bacterial cell wall. Cell lysis is subsequently mediated by bacterial cell wall autolysins (such as autolysins); Mezlocillin may interfere with autolysin inhibitors.

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Pharmacodynamics
Mezlocillin is a penicillin-type β-lactam antibiotic used to treat bacterial infections caused by susceptible bacteria, typically Gram-positive bacteria. The name "penicillin" can refer to several existing penicillin derivatives or to a class of antibiotics derived from penicillin. Mezlocillin exhibits in vitro activity against Gram-positive, Gram-negative aerobic, and anaerobic bacteria. Mezlocillin's bactericidal activity stems from its inhibition of cell wall synthesis and its action through binding to penicillin-binding proteins (PBPs). Mezlocillin is stable against the hydrolytic activity of various β-lactamases, including penicillinase, cephalosporinase, and extended-spectrum β-lactamases. Mezlocillin can be used to treat Mezlocillin-sensitive strains of Haemophilus influenzae, Klebsiella spp., Pseudomonas spp., Proteus mirabilis, and Escherichia coli. Escherichia coli, Enterobacter spp., Enterococcus faecalis, Peptococcus spp., Peptostreptococcus spp., Bacteroides spp. (including Bacteroides fragilis), Morganella morganii, Serratia spp., Neisseria gonorrhoeae, Proteus vulgaris, and Providencia reticularis. This drug has been discontinued in the United States.

C21H25N5O8S2

539.581902265549

539.114

51481-65-3

Mezlocillin sodium;42057-22-7

656511

Typically exists as solid at room temperature

1.6±0.1 g/cm3

655.5ºC at 760 mmHg

350.2ºC

1.701

-1.18

207.18

3

9

6

36

1080

4

O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC([C@H](NC(N3CCN(S(=O)(C)=O)C3=O)=O)C4=CC=CC=C4)=O)N1C2=O)O

YPBATNHYBCGSSN-VWPFQQQWSA-N

InChI=1S/C21H25N5O8S2/c1-21(2)14(18(29)30)26-16(28)13(17(26)35-21)22-15(27)12(11-7-5-4-6-8-11)23-19(31)24-9-10-25(20(24)32)36(3,33)34/h4-8,12-14,17H,9-10H2,1-3H3,(H,22,27)(H,23,31)(H,29,30)/t12-,13-,14+,17-/m1/s1

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

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。