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SKU	北京总部	北京海淀	武汉	广州
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SKU

北京总部

北京海淀

武汉

广州

IT0330-10mg

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CAS	No.32986-56-4
中文名称	妥布霉素
英文名称	Tobramycin
别名	Deoxykanamycin B;Nebramycin Factor 6;NSC 180514
分子式	C₁₈H₃₇N₅O₉
分子量	467.51
溶解性	Soluble in Water ≥10mg/mL
酶活/效价	≥900μg/mg
外观(性状)	White to off-white Solid
储存条件	Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
EC	EINECS 251-322-5
MDL	MFCD00077885
SMILES	O[C@@H]([C@@H]1O[C@@]([C@@H](C[C@@H]2O)N)([H])O[C@@H]2CN)[C@H]([C@@H](C[C@@H]1N)N)O[C@@]([C@@H]([C@@H](N)[C@@H]3O)O)([H])O[C@@H]3CO
InChIKey	NLVFBUXFDBBNBW-PBSUHMDJSA-N
InChI	InChI=1S/C18H37N5O9/c19-3-9-8(25)2-7(22)17(29-9)31-15-5(20)1-6(21)16(14(15)28)32-18-13(27)11(23)12(26)10(4-24)30-18/h5-18,24-28H,1-4,19-23H2/t5-,6+,7+,8-,9+,10+,11-,12+,13+,14-,15+,16-,17+,18+/m0/s1
PubChem CID	36294
靶点	Antibiotic
通路	Anti-infection
背景说明	Tobramycin是氨基糖苷类广谱抗生素。
生物活性	Tobramycin (Nebramycin Factor 6) is a parenterally administered， broad spectrum aminoglycoside antibiotic that is widely used in the treatment of moderate to severe bacterial infections due to sensitive organisms[1].Tobramycin can be used to pneumonia research caused by Pseudomonas aeruginosa[2][3].
In Vitro	We previously identified an Enzyme， PodA， that demethylated pyocyanin and disrupted P. aeruginosa biofilm development in vitro. Here， we asked if this protein could be used as a potential therapeutic for P. aeruginosa infections together with tobramycin， an Antibiotic typically used in the clinic. A major roadblock to answering this question was the poor yield and stability of wild-type PodA purified from standard Escherichia coli overexpression systems.We hypothesized that the insufficient yields were due to poor packing within PodAs obligatory homotrimeric interfaces. We therefore applied the protein design algorithm， AffiLib， to optimize the symmetric core of this interface， resulting in a design that incorporated five mutations leading to a 20-fold increase in protein yield from heterologous expression and purification and a substantial increase in stability to environmental conditions.The addition of the designed PodA with tobramycin led to increased killing of P. aeruginosa cultures under oxic and hypoxic conditions in both the planktonic and biofilm states.[2]。Cell Viability Assay[2]Cell Line:Pseudomonas aeruginosa；Concentration: 2，10，50 ng/mL；Incubation Time:24 h；Result:Greatly decreased cell viability compared to no protein or inactive mycobacterium fortuitum enzyme (PodA) controls while PodA10 alone did not increase cell death.
In Vivo	The purpose of these experiments was to evaluate combination chemotherapy with meropenem plus tobramycin for P. aeruginosa in a murine pneumonia model. Neutropenia was induced by cyclophosphamide. Pharmacokinetics of meropenem and tobramycin were determined using a population pharmacokinetic approach. Both drugs were given at 4 - h intervals. Meropenem was administered as total daily doses of 30 to 600 mg/kg of body weight， while tobramycin doses ranged from 50 to 400 mg/kg. Combination therapy evaluated all combinations of 50， 100， and 150 mg/kg/day of tobramycin doses with 60 or 300 mg/kg/day of meropenem. Total and drug - resistant organisms were enumerated.[3]Animal Model: Murine Model of Pseudomonas aeruginosa Pneumonia Female， Swiss-Webster mice [3]；Dosage:50， 100， 150， 214， and 400 mg/kg/day；Administration:Intraperitoneal injection (i.p.) ，once every 4h；Result:Had near-maximal killing of the wild-type bacteria occurred at approximately 150 mg/kg/day when tobramycin alone.Combinated with Meropenem (HY-13678) produced near-maximal effect (i.e.， bacterial cell kill) at low doses of both drugs (60 and 50 mg/kg/day for Meropenem (HY-13678) and tobramycin， respectively).Animal Model: Mice， rats， cats and dogs for toxicologic evaluation[4]；Dosage:7.5，15，30，120，441，969 mg/kg；Administration:Subcutaneous injection (s.c.)， Intravenous injection (i.v.) ，Intramuscular injection(i.m.)；Result: The s.c. LD50 values in mice and rats were 441 and 969 mg/kg， respectively.Within 1 hour after treated， death with central nervous system depression as a precursor occurred in rats and mice.A 100 mg/kg iv dose in chloraloseanesthetized catsproduced a moderate， transient decreasein blood pressure and a significant decrease in inspiratory volume and soleus twitch force.Changed renal tissue in rats which were given daily sc doses of 15-120 mg/kg for 3 months.im dose of 7.5 mg/kg for a l-month had no apparent effect on dogs， but a 30 mg/kg dose for a l-month produced severerenal damage.
数据来源文献	[1]. Tobramycin. [2]. VanDrisse CM， et.al. Computationally designed pyocyanin demethylase acts synergistically with tobramycin to kill recalcitrant Pseudomonas aeruginosa biofilms. Proc Natl Acad Sci U S A. 2021 Mar 23;118(12):e2022012118. [3]. Louie A， et.al. Impact of meropenem in combination with tobramycin in a murine model of Pseudomonas aeruginosa pneumonia. Antimicrob Agents Chemother. 2013 Jun;57(6):2788-92. [4]. Welles JS， et.al. Preclinical toxicology studies with tobramycin. Toxicol Appl Pharmacol. 1973 Jul;25(3):398-409.
规格	10mg 50mg
单位	瓶