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328898-40-4
  • names:

    Tildipirosin

  • CAS号:

    328898-40-4

    MDL Number: MFCD13194925
  • MF(分子式): C41H71N3O8 MW(分子量): 734.018
  • EINECS: Reaxys Number:
  • Pubchem ID:24860548 Brand:BIOFOUNT
泰地罗新
泰地罗新(328898-40-4,Tildipirosin)是用于兽医学的新型16元环大环内酯类药物。Tildipirosin可治疗引起牛和猪呼吸道感染的细菌性病原体,包括溶血曼海姆氏菌和多杀巴斯德氏菌(BRD牛呼吸道疾病)。
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中文别名 泰地罗新(328898-40-4);替比罗定;替匹罗星;20,23-二哌啶基-mycaminosyl-tylonolide;替地吡辛;
英文别名 Tildipirosin(328898-40-4);20,23-dipiperidinyl-mycaminosyl-tylonolide;tildipirosin;Zuprevo; 20-Deoxo-23-deoxy-5-O- [3,6-dideoxy-3-(dimethylamino)-β-D-glucopyranosyl] -20,23-di-1-piperidinyltylonolide;
CAS号 328898-40-4
SMILES CC[C@@H]1[C@H](/C=C(/C=C/C(=O)[C@@H](C[C@@H]([C@@H]([C@H]([C@@H](CC(=O)O1)O)C)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)C)O)N(C)C)O)CCN3CCCCC3)C)\C)CN4CCCCC4
Inchi InChI=1S/C41H71N3O8/c1-8-35-32(26-44-20-13-10-14-21-44)23-27(2)15-16-33(45)28(3)24-31(17-22-43-18-11-9-12-19-43)40(29(4)34(46)25-36(47)51-35)52-41-39(49)37(42(6)7)38(48)30(5)50-41/h15-16,23,28-32,34-35,37-41,46,48-49H,8-14,17-22,24-26H2,1-7H3/b16-15+,27-23+/t28-,29+,30-,31+,32-,34-,35-,37+,38-,39-,40-,41+/m1/s1
InchiKey HNDXPZPJZGTJLJ-UEJFNEDBSA-N
分子式 Formula C41H71N3O8
分子量 Molecular Weight 734.018
闪点 FP 465.9±34.3 °C
熔点 Melting point >110°C (dec.)
沸点 Boiling point 846.8±65.0 °C at 760 mmHg
Polarizability极化度 81.2±0.5 10-24cm3
密度 Density 1.2±0.1 g/cm3
蒸汽压 Vapor Pressure 0.0±0.6 mmHg at 25°C
溶解度Solubility 生物体外In Vitro:DMSO溶解度≥ 100 mg/mL(136.24 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状 白色固体
储藏条件 Storage conditions -20°摄氏度 Freezer

泰地罗新(328898-40-4,Tildipirosin)实验注意事项
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:泰地罗新试剂,泰地罗新杂质,泰地罗新合成,泰地罗新中间体,泰地罗新密度,泰地罗新溶解度,泰地罗新旋光度,泰地罗新闪点,泰地罗新熔点,泰地罗新购买,泰地罗新MSDS,

产品说明 泰地罗新(328898-40-4,Tildipirosin)可以作为药物杂质对照品以及生物医药类试剂。
Introduction泰地罗新(328898-40-4,Tildipirosin)can be used as a reference substance for drug impurities and reagents,only for research.
Application1
Application2
Application3
泰地罗新(328898-40-4,Tildipirosin)药理学:
Tildipirosin是用于兽医学的新型16元环大环内酯类药物。Tildipirosin可治疗引起牛和猪呼吸道感染的细菌性病原体,包括溶血曼海姆氏菌和多杀巴斯德氏菌(BRD牛呼吸道疾病)。
警示图
危险性 warning
危险性警示 Not available
安全声明 H303+H313+H333
安全防护 P264+P280+P305+P351+P338+P337+P313
备注 实验过程中防止吸入、食入,做好安全防护
泰地罗新(328898-40-4,Tildipirosin)危害标识:
象形图
信号 Warning
GHS危险说明 Aggregated GHS information provided by 12 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]
H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]
H373 (100%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]
Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码 P201, P202, P260, P261, P272, P280, P281, P302+P352, P308+P313, P314, P321, P333+P313, P363, P405, and P501
(The corresponding statement to each P-code can be found at the GHS Classification page.)
 
A randomised clinical trial of a metaphylactic treatment with tildipirosin for bovine respiratory disease in veal calves,BMC Veterinary Research[DOI: 10.1186s12917-017-1097-1]
Rose M, et al. A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs. J Vet Pharmaco
Angell JW, et al. In vitro susceptibility of contagious ovine digital dermatitis associated Treponema spp. isolates to antimicrobial agents in the UK. Vet Dermatol. 2015 Dec;26(6):484-7, e114-5.
Confer AW, et al. Clinical disease and lung lesions in calves experimentally inoculated with Histophilus somni five days after metaphylactic administration of tildipirosin or tulathromycin. Am J Vet R
Michael GB, et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. J Antimicrob Che
泰地罗新(328898-40-4,Tildipirosin)参考文献:
1.A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs.
Rose M1, Pridmore A2, Shaw A2, Wilhelm C1, Menge M1, Kilp S1, Röpke R1, Nürnberger M. J Vet Pharmacol Ther. 2016 Jun;39(3):277-86. doi: 10.1111/jvp.12277. Epub 2015 Nov 5.

Tildipirosin (TIP) is a novel 16-membered-ring macrolide authorized for the treatment of bovine and swine respiratory disease. The pH dependency of macrolide antimicrobial activity is well known. Considering that the pH in the colon contents of growing beef cattle and pigs is usually below pH 7.0, the minimum inhibitory concentrations (MIC) of TIP against foodborne bacterial pathogens such as Campylobacter (C.) coli, C. jejuni and Salmonella enterica and commensal species including Enterococcus (E.) faecalis, E. faecium and Escherichia coli were determined under standard (pH 7.3 ± 1) or neutral as well as slightly acidic conditions. A decrease in pH from 7.3 to 6.7 resulted in an increase in MICs of TIP. Except for the MICs > 256 μg/mL observed in the resistant subpopulation of the C. coli and the Enterococcus species, the MIC ranges increased from 2-8 μg/mL to 64-> 256 μg/mL for Salmonella enterica and E. coli, from 8-16 μg/mL to 32-128 μg/mL for the two Campylobacter species, and from 4-32 μg/mL to 128-> 256 μg/mL for both Enterococcus species.

2.Pulmonary lesions and clinical disease response to Mannheimia haemolytica challenge 10 days following administration of tildipirosin or tulathromycin.
Amrine DE1, White BJ, Larson RL, Mosier DA. J Anim Sci. 2014 Jan;92(1):311-9. doi: 10.2527/jas.2013-6577. Epub 2013 Nov 15.

This clinical trial evaluated the impact of metaphylactic antimicrobial administration 10 d before experimental inoculation with Mannheimia haemolytica (MH) to mitigate pulmonary lesions. Thirty-three crossbreed heifers were procured as a single group and were randomly allocated to 1 of 3 blocks and to treatment, tildipirosin (ZUP; 4 mg/kg) or tulathromycin (DRX; 2.5 mg/kg) or saline (SAL; 1 mL/45.5 kg), within block on arrival at Kansas State University. All trial procedures were staggered by 7-d intervals for each block, resulting in all animals within a block receiving treatment, challenge, and necropsy on the same dates. Heifers within each block received an endoscopic MH challenge 10 d following treatment administration (d 0) and were housed in individual indoor stalls for 3 d postchallenge. Clinical illness scores (CIS), respiration quality scores, appetite scores, and injection site reactions were recorded on all animals from d 0 through d 13.

3.Overall decrease in the susceptibility of Mycoplasma bovis to antimicrobials over the past 30 years in France.
Gautier-Bouchardon AV1, Ferré S1, Le Grand D2, Paoli A2, Gay E3, Poumarat F2. PLoS One. 2014 Feb 4;9(2):e87672. doi: 10.1371/journal.pone.0087672. eCollection 2014.

Mycoplasma (M.) bovis is frequently implicated in respiratory diseases of young cattle worldwide. Today, to combat M. bovis in Europe, only antimicrobial therapy is available, but often fails, leading to important economical losses. The antimicrobial susceptibility of M. bovis is not covered by antimicrobial resistance surveillance networks. The objectives of this study were to identify resistances that were acquired over the last 30 years in France and to determine their prevalence within contemporary strains. The minimum inhibition concentration (MIC) values of 12 antimicrobials, considered active on M. bovis, were compared, using an agar dilution method, between 27 and 46 M. bovis isolates respectively obtained in 1978-1979 and in 2010-2012 from 73 distinct respiratory disease outbreaks in young cattle all over France. For eight antimicrobials, resistances were proven to be acquired over the period and expressed by all contemporary strains.

4.[New drugs for horses and production animals in 2011].
Emmerich IU1. Tierarztl Prax Ausg G Grosstiere Nutztiere. 2012 Oct 17;40(5):301-8.

In 2011, three newly developed active pharmaceutical ingredients for horses and food producing animals were released on the German market for veterinary drug products. Two of these new products represent different drug classes of antibiotics, the polypeptide antibiotic Bacitracin (Bacivet™) and the macrolide antibiotic Clorsulon (Levatum®). The third product represents an anticestodal antiparasitic (Tildipirosin, Zuprevo®). Furthermore, three established veterinary active pharmaceutical ingredients were modified to allow their application for additional species. Thus the nonsteroidal anti-inflammatory drug sodium salicylate is now additionally authorised for turkeys and both the macrolide antibiotic Tilmicosin and the anticoccidial drug Toltrazuril are currently available for sheep. Additionally, two veterinary drugs with a new formulation as well as a veterinary drug for horses and food producing animals with a resourceful new combination of active pharmaceutical ingredients have recently been released.
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