规格 | 价格 | 库存 | 数量 |
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100mg |
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Other Sizes |
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体外研究 (In Vitro) |
青霉素 V (0.002-8.0 mg/L) 在最低抑制浓度 (MIC) 0.004-0.008 mg/L 时即可抑制链球菌生长[2]。青霉素 V (0.002-8.0 mg/L) 的 MIC90 为 8 mg/L,可以阻止艰难梭菌生长[3]。青霉素 V(0.004-0.063 mg/L;18 小时)的 MIC 为 0.016 mg/L,可抑制金黄色葡萄球菌的生长 [4]。
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体内研究 (In Vivo) |
在小鼠大腿肌肉中,青霉素 V(0.063-0.25 mg/kg;单次皮下注射)可抑制金黄色葡萄球菌生长 [4]。患有急性化脓性中耳炎(AOM)的大鼠可以通过口服青霉素V(100 mg/kg),每天一次,持续五天来避免暴发性感染[5]。青霉素V(2 mg/kg;单次皮下注射)的平均曲线下面积(AUC)为0.47 mg/L·h,血浆半衰期为61分钟[4][4]。
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动物实验 |
Animal/Disease Models: Specific pathogen-free (SPF) male Swiss mice (20-25 g) inoculated with Staphylococcus aureus [4]
Doses: 0.063, 0.13, 0.25 mg/kg Route of Administration: Single subcutaneous injection Experimental Results: Reduction in CFU number ( 1.34 × 107 counts/mL) compared with the control at a dose of 0.25 mg/kg (3.5 × 107 counts/mL). |
药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
A dose of 1,000,000 units of the acid gives peak plasma levels of about 2 to 3 ug/ml, but the potassium salt will provide levels of 4.5 to 9 ug/ml. Penicillin VK provides faster and higher blood levels of antibiotic than Penicillin V. Biological Half-Life The half-life is 0.5 to 0.6 hr. |
毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited information indicates that penicillin V 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. Penicillin V is acceptable in nursing mothers. ◉ Effects in Breastfed Infants In one study, 12 infants were breastfed during maternal penicillin V therapy. Seven appeared normal, 3 had looser stools than normal, and 1 had a rash on the buttocks on the last day of therapy. These effects were possibly related to penicillin V in milk, but no control group was present. One infant had stains of blood in the stool, but it had happened once prior to maternal penicillin V treatment. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
参考文献 |
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其他信息 |
Penicillin vk+ is an odorless white crystalline powder. Slightly bitter taste. pH (0.5% aqueous solution) 5 to 7.5. (NTP, 1992)
Phenoxymethylpenicillin potassium is an organic potassium salt. It contains a phenoxymethylpenicillin(1-). Penicillin V Potassium is the potassium salt of penicillin V, a member of the penicillin antibiotic family with broad-spectrum bactericidal activity. Penicillin V binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms. See also: Penicillin V (has active moiety). Mechanism of Action The penicillins and their metabolites are potent immunogens because of their ability to combine with proteins and act as haptens for acute antibody-mediated reactions. The most frequent (about 95 percent) or "major" determinant of penicillin allergy is the penicilloyl determinant produced by opening the beta-lactam ring of the penicillin. This allows linkage of the penicillin to protein at the amide group. "Minor" determinants (less frequent) are the other metabolites formed, including native penicillin and penicilloic acids. /Penicillins/ Bactericidal; inhibit bacterial cell wall synthesis. Action is dependent on the ability of penicillins to reach and bind penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Penicillin-binding proteins (which include transpeptidases, carboxypeptidases, and endopeptidases) are enzymes that are involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Penicillins bind to, and inactivate, penicillin-binding proteins, resulting in the weakening of the bacterial cell wall and lysis. /Penicillins/ |
分子式 |
C16H17KN2O5S
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分子量 |
388.4793
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精确质量 |
388.049
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CAS号 |
132-98-9
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相关CAS号 |
Penicillin V-d5;1356837-87-0;Penicillin V;87-08-1;Penicillin V-13C6 potassium;Penicillin V Potassium-d5;2699607-22-0
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PubChem CID |
23676814
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外观&性状 |
White to off-white solid powder
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密度 |
1.40
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沸点 |
681.4ºC at 760 mmHg
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熔点 |
197-202°C
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闪点 |
365.9ºC
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蒸汽压 |
1.69E-19mmHg at 25°C
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tPSA |
124.07
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氢键供体(HBD)数目 |
1
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氢键受体(HBA)数目 |
6
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可旋转键数目(RBC) |
5
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重原子数目 |
25
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分子复杂度/Complexity |
553
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定义原子立体中心数目 |
3
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SMILES |
CC1([C@@H](N2[C@H](S1)[C@@H](C2=O)NC(=O)COC3=CC=CC=C3)C(=O)[O-])C.[K+]
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InChi Key |
HCTVWSOKIJULET-LQDWTQKMSA-M
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InChi Code |
InChI=1S/C16H18N2O5S.K/c1-16(2)12(15(21)22)18-13(20)11(14(18)24-16)17-10(19)8-23-9-6-4-3-5-7-9;/h3-7,11-12,14H,8H2,1-2H3,(H,17,19)(H,21,22);/q;+1/p-1/t11-,12+,14-;/m1./s1
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化学名 |
potassium;(2S,5R,6R)-3,3-dimethyl-7-oxo-6-[(2-phenoxyacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
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别名 |
Penicillin V potassium HSDB 6315 Penicillin VK
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HS Tariff Code |
2934.99.9001
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存储方式 |
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,避免吸湿/受潮。 |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ~12 mg/mL (~30.89 mM)
H2O : ~6 mg/mL (~15.44 mM) |
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 1.2 mg/mL (3.09 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 12.0 mg/mL澄清DMSO储备液加入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。 配方 2 中的溶解度: ≥ 1.2 mg/mL (3.09 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 12.0 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。 View More
配方 3 中的溶解度: ≥ 1.2 mg/mL (3.09 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。 配方 4 中的溶解度: 100 mg/mL (257.41 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. 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。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5741 mL | 12.8707 mL | 25.7414 mL | |
5 mM | 0.5148 mL | 2.5741 mL | 5.1483 mL | |
10 mM | 0.2574 mL | 1.2871 mL | 2.5741 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05082909 | UNKNOWN STATUS | Drug: Probenecid | Infection, Bacterial | Imperial College London | 2021-12-21 | Phase 1 Phase 2 |
NCT03208361 | TERMINATED | Drug: Penicillin V Drug: Amoxicillin |
Community-acquired Pneumonia (CAP) | Fundacio d'Investigacio en Atencio Primaria Jordi Gol i Gurina | 2013-11-05 | Phase 3 |
NCT00823433 | TERMINATED | Drug: oral penicillin V | Group B Streptococcus | William Beaumont Hospitals | 2009-01 | Early Phase 1 |
NCT02188472 | COMPLETED | Drug: Penicillin V Drug: Trimethoprim Drug: Placebo |
Oxidative Stress | Henrik Enghusen Poulsen | 2010-11 | Phase 1 |
NCT04083417 | UNKNOWN STATUS | Drug: Phenoxymethylpenicillin Other: No antibiotic treatment |
Sore Throat Tonsillitis |
Katarina Hedin | 2019-09-09 | Phase 4 |