在0.05～1μg/mL的最低抑菌浓度（MIC）下，头孢氯定可抑制以下病原菌：金黄色葡萄球菌、青霉素敏感菌株和青霉素耐药菌株、化脓性链球菌、肺炎链球菌、白喉棒状杆菌、败血梭菌等。 1]。

在兔子和猴子中，头孢氯定（50-500 mg/kg；肌肉注射）显示出剂量相关的肾毒性[2]。

Animal/Disease Models: Rabbits and monkeys [2]
Doses: 50, 100, 200 and 500 mg/kg
Route of Administration: intramuscularinjection
Experimental Results: 200 and 500 mg/kg caused significant changes in renal function and proximal tubule necrosis. Renal impairment does not appear to occur at doses of 50 and 100 mg/kg.

Absorption, Distribution and Excretion
Renal.
.../CEPHALORIDINE/ POORLY ABSORBED FROM GI TRACT. PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED; 10 TO 20% OF PLASMA CEPHALORIDINE IS BOUND TO PROTEIN.
IM INJECTIONS OF 0.5 & 1 G YIELD PEAK PLASMA CONCN OF 15 & 30 UG/ML, RESPECTIVELY. APPROX 75% OF GIVEN DOSE IS EXCRETED IN URINE, MAINLY BY GLOMERULAR FILTRATION. CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH...
PLACENTAL DRUG TRANSFER- CEPHALORIDINE: TIME TO APPEAR IN FETUS 30 MIN; TIME TO FETAL/MATERNAL CONCN EQUIL 5 HR. /FROM TABLE/
.../CEPHALORIDINE/ READILY PENETRATE NORMAL EYE FOLLOWING SYSTEMIC OR SUBCONJUNCTIVAL ADMIN...
...CEPHALORIDINE...SHOWN...TO PENETRATE INTO BONE TO VERY LIMITED EXTENT AFTER SC OR ORAL DOSES TO RATS. RATIOS OF BONE TO SERUM CONCN AVG...1:7 FOR CEPHALORIDINE...DURING 0.25-4 HR AFTER DOSING.

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Biological Half-Life
.../CEPHALORIDINE/ PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED... WHILE ITS T/2 (60 TO 90 MIN)...ONLY SMALL AMT ARE DETECTABLE AFTER 8 HR.
/IN RATS/ RATIOS OF BONE TO SERUM CONCN AVG...1:7 FOR CEPHALORIDINE...DURING 0.25-4 HR AFTER /ORAL OR SC/ DOSING. DESPITE DIFFERENCES IN CONCN, T/2 IN BONE & SERUM WERE SIMILAR.

Interactions
NON-IONIC, ANIONIC, & ZWITTERIONIC SURFACTANTS INDUCED RAPIDLY REVERSIBLE HYPER-ABSORPTIVE STATE IN THOMAS CANINE FUNDIC POUCH FOR CEPHALORIDINE...BLOOD LEVELS...MANY TIMES GREATER THAN VALUES IN CONTROLS.
CEPHALORIDINE SEEMS TO HAVE GREATEST POTENTIAL FOR NEPHROTOXICITY.../IT SHOULD NOT/ BE USED WITH GENTAMICIN /OR OTHER AMINOGLYCOSIDES, AMIKACIN, NEOMYCIN, PAROMOMYCIN & TOBRAMYCIN/ UNLESS LIFE-THREATENING CONDITION EXISTS /MAY INCR NEPHROTOXICITY/.
CEPHALORIDINE NEPHROTOXICITY IS ENHANCED BY CONCURRENT FUROSEMIDE ADMIN. SUCH THERAPY SHOULD BE AVOIDED IN PATIENTS WHO HAVE EVEN MILD PREEXISTING RENAL DISEASE.
...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF PROBENECID OR SULFINPYRAZONE. DIMINISHED TUBULAR SECRETION OF...WEAK ACIDS COULD RESULT IN HIGHER & MORE SUSTAINED SERUM LEVELS & HENCE, INTENSIFICATION OF DRUG ACTIVITY. /CEPHALOSPORINS/
Groups of ten male rats were treated with a high challenge dose of cephaloridine (3750 mg/kg), with methylprednisolone (100 mg/kg) or with cephaloridine and methylprednisolone by single sc injection. A control group received the injection vehicles only. Urine was collected from all animals daily over 18-hr collection periods, up to 96 hr after treatment. Blood was collected at 24, 48, 72 and 96 hr after treatment. At necropsy, kidneys were weighed, processed and examined histopathologically. Results show that methylprednisolone significantly ameliorated the nephrotoxicity of the challenge dose of cephaloridine. Cephaloridine-only treated rats had severe toxic nephrosis characterized by acute tubular necrosis, and elevated blood urea and creatinine. by contrast, the majority of cephaloridine plus methylprednisolone treated rats had only a slight or moderate toxic nephrosis, and had lower blood urea and creatinine levels compared with rats treated with cephaloridine only, indicating preservation of kidney function. Interestingly, rats treated with cephaloridine and methylprednisolone had higher urinary enzymes ... as well as protein and glucose, compared with rats treated with cephaloridine only. this is taken to indicate that rats treated with cephaloridine only had such marked kidney damage and necrosis that the population of cells able to produce these marker enzymes was significantly and rapidly depleted, but the protection afforded by methylprednisolone allowed cephaloridine plus methylprednisolone treated rats to sustain urinary enzyme output. Effects on urinary glucose and other parameters ... demonstrate interactions between glucocorticoid pharmacology and cephaloridine nephrotoxicity.

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Non-Human Toxicity Values
LD50 MOUSE ORAL GREATER THAN 15 G/KG
LD50 MONKEY INTRAMUSCULAR GREATER THAN 0.2 G/KG

[1]. P. W. Muggleton, et al. Laboratory Evaluation of a New Antibiotic-Cephaloridine (Ceporin). Br Med J. 1964 Nov 14;2(5419):1234-7.
[2]. Perkins RL, et al. Cephaloridine and cephalothin: comparative studies of potential nephrotoxicity. J Lab Clin Med. 1968 Jan;71(1):75-84.

Cefaloridine is a cephalosporin compound having pyridinium-1-ylmethyl and 2-thienylacetamido side-groups. A first-generation semisynthetic derivative of cephalosporin C. It has a role as an antibacterial drug. It is a cephalosporin, a semisynthetic derivative and a beta-lactam antibiotic allergen.
Cephaloridine or cefaloridine is a first generation semisynthetic cephalosporin. It is derived from cephalosporin C and is a zwitterion at physiological pH.
Cephaloridine is a semisynthetic, broad-spectrum, first-generation cephalosporin with antibacterial activity. Cephaloridine binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
A cephalosporin antibiotic.

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Mechanism of Action
CEPHALOTHIN & ITS CONGENERS INHIBIT BACTERIAL CELL-WALL SYNTHESIS IN MANNER SIMILAR TO THAT OF PENICILLIN. /CEPHALOSPORINS/
Cephaloglycin and cephaloridine are acutely toxic to the proximal renal tubule, in part because of their cellular uptake by a contraluminal anionic secretory carrier and in part through their intracellular attack on the mitochondrial transport and oxidation of tricarboxylic acid (TCA) cycle anionic substrates. Preliminary studies with cephaloglycin have provided evidence of a role of fatty acid (FA) metabolism in its nephrotoxicity, and work with cephaloridine has shown it to be a potent inhibitor of renal tubular cell and mitochondrial carnitine (Carn) transport.

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Therapeutic Uses
Cephalosporins
GENERAL RANGE OF ACTIVITY & ANTIBACTERIAL SPECTRUM OF CEPHALORIDINE CLOSELY APPROX THAT OF CEPHALOTHIN, ALTHOUGH SOME STRAINS OF E COLI MAY BE SOMEWHAT MORE SENSITIVE TO FORMER. IT ALSO APPEARS TO BE MORE ACTIVE THAN CEPHALOTHIN AGAINST CL PERFRINGENS (WELCHII). MYCOBACTERIUM FORTUITUM IS SENSITIVE TO CEPHALORIDINE...
CEPHALORIDINE...GIVEN PARENTERALLY & SUBCONJUNCTIVALLY TO TREAT INTRAOCULAR INFECTIONS & MAY BE ADMIN TOPICALLY & SUBCONJUNCTIVALLY TO TREAT CORNEAL ULCERS.
CEPHALORIDINE IS EFFECTIVE IN THERAPY OF BRONCHITIS DUE TO H INFLUENZAE, BUT OTHER AGENTS OFTEN PRODUCE BETTER RESULTS, THIS DRUG HAS ALSO BEEN FOUND USEFUL WHEN EMPLOYED AS AEROSOL IN PATIENT WITH PURULENT BRONCHITIS.
For more Therapeutic Uses (Complete) data for CEPHALORIDINE (10 total), please visit the HSDB record page.

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Drug Warnings
CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH; SINGLE DOSE OF 1 G IM YIELDS DETECTABLE CONCN FOR AS LONG AS 4 DAYS. ...CEPHALORIDINE SHOULD NOT BE GIVEN TO SUCH PATIENTS, SINCE IT IS NEPHROTOXIC.
WHILE CEPHALORIDINE PRODUCES LESS IRRITATION /THAN CEPHALOTHIN/, ITS NEPHROTOXICITY OUTWEIGHS THIS ADVANTAGE.
IN 48-HR HUMAN INFANTS...CEPHALORIDINE...HAVE VERY LONG PLASMA T/2, & TOXIC CONCN ARE REACHED WHEN DOSES ARE LOWERED CONSIDERABLY.
CEPHALORIDINE IS INJECTED EITHER IM OR IV. ... SINCE OTHER, LESS TOXIC CEPHALOSPORINS ARE AVAIL, THERE IS NO REASON TO RECOMMEND THIS PREPN.
For more Drug Warnings (Complete) data for CEPHALORIDINE (7 total), please visit the HSDB record page.

C19H17N3O4S2

415.482

415.066

50-59-9

Cephaloridine hydrate;102039-86-1

5773

CRYSTALS
WHITE TO OFF-WHITE, CRYSTALLINE POWDER

184°C

0.011

146.96

1

6

5

28

687

2

O=C([O-])C=1N2C([C@@H](NC(CC3=CC=CS3)=O)[C@H]2SCC1C[N+]4=CC=CC=C4)=O

CZTQZXZIADLWOZ-CRAIPNDOSA-N

InChI=1S/C19H17N3O4S2/c23-14(9-13-5-4-8-27-13)20-15-17(24)22-16(19(25)26)12(11-28-18(15)22)10-21-6-2-1-3-7-21/h1-8,15,18H,9-11H2,(H-,20,23,25,26)/t15-,18-/m1/s1

(6R,7R)-8-oxo-3-(pyridin-1-ium-1-ylmethyl)-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

Cefaloridine; Cephaloridine; Sch 11527

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。