Tilmicosin phosphate
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MedKoo CAT#: 462733

CAS#: 137330-13-3 (phosphate)

Description: Tilmicosin is a macrolide antibiotic that inhibits protein synthesis in bacteria. It prevents the growth of M. haemolytica, P. multocida, and E. coli with MIC values of 2-4 µM and is commonly used against respiratory infections in swine and cattle.

Chemical Structure

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Tilmicosin phosphate
CAS# 137330-13-3 (phosphate)
Instruction

Theoretical Analysis

MedKoo Cat#: 462733
Name: Tilmicosin phosphate
CAS#: 137330-13-3 (phosphate)
Chemical Formula: C46H83N2O17P
Exact Mass: 966.54
Molecular Weight: 967.141
Elemental Analysis: C, 57.13; H, 8.65; N, 2.90; O, 28.12; P, 3.20

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100mg USD 250 2 Weeks
500mg USD 550 2 Weeks
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Related CAS #: 137330-13-3 (phosphate)   108050-54-0 (free base)  

Synonym: Micotil 300; Pulmotil 90; LY177370 phosphate; LY-177370 phosphate; LY 177370 phosphate; EL-870 phosphate; EL870 phosphate; EL 870 phosphate

IUPAC/Chemical Name: (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-(((2R,3R,4S,5S,6R)-4-(dimethylamino)-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-7-(2-((3R,5S)-3,5-dimethylpiperidin-1-yl)ethyl)-16-ethyl-4-hydroxy-15-((((2R,3R,4R,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)methyl)-5,9,13-trimethyloxacyclohexadeca-11,13-diene-2,10-dione phosphate

InChi Key: NESIVXZOSKKUDP-ARVJLQODSA-N

InChi Code: InChI=1S/C46H80N2O13.H3O4P/c1-13-36-33(24-57-46-44(56-12)43(55-11)40(53)31(8)59-46)19-25(2)14-15-34(49)28(5)20-32(16-17-48-22-26(3)18-27(4)23-48)42(29(6)35(50)21-37(51)60-36)61-45-41(54)38(47(9)10)39(52)30(7)58-45;1-5(2,3)4/h14-15,19,26-33,35-36,38-46,50,52-54H,13,16-18,20-24H2,1-12H3;(H3,1,2,3,4)/b15-14+,25-19+;/t26-,27+,28-,29+,30-,31-,32+,33-,35-,36-,38+,39-,40-,41-,42-,43-,44-,45+,46-;/m1./s1

SMILES Code: CC[C@H]1OC(C[C@H]([C@@H]([C@H]([C@H](C[C@H](C(/C=C/C(C)=C/[C@@H]1CO[C@@H]2O[C@@H]([C@H]([C@H]([C@H]2OC)OC)O)C)=O)C)CCN3C[C@@H](C[C@@H](C3)C)C)O[C@@H]4O[C@@H]([C@H]([C@H](N(C)C)[C@H]4O)O)C)C)O)=O.OP(O)(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 967.14 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Oda SS, Derbalah AE. Impact of Diclofenac Sodium on Tilmicosin-Induced Acute Cardiotoxicity in Rats (Tilmicosin and Diclofenac Cardiotoxicity). Cardiovasc Toxicol. 2018 Feb;18(1):63-75. doi: 10.1007/s12012-017-9414-2. PMID: 28593443.

2: Zhu L, Cao X, Xu Q, Su J, Li X, Zhou W. Evaluation of the antibacterial activity of tilmicosin-SLN against Streptococcus agalactiae: in vitro and in vivo studies. Int J Nanomedicine. 2018 Aug 17;13:4747-4755. doi: 10.2147/IJN.S168179. PMID: 30147316; PMCID: PMC6103319.

3: Fittipaldi N, Klopfenstein C, Gottschalk M, Broes A, Paradis MA, Dick CP. Assessment of the efficacy of tilmicosin phosphate to eliminate Actinobacillus pleuropneumoniae from carrier pigs. Can J Vet Res. 2005 Apr;69(2):146-50. PMID: 15971680; PMCID: PMC1142183.

4: Song M, Li Y, Fai C, Cui S, Cui B. The controlled release of tilmicosin from silica nanoparticles. Drug Dev Ind Pharm. 2011 Jun;37(6):714-8. doi: 10.3109/03639045.2010.538059. Epub 2011 Jan 5. PMID: 21204738.

5: Blondeau JM, Shebelski SD, Hesje CK. Bactericidal effects of various concentrations of enrofloxacin, florfenicol, tilmicosin phosphate, and tulathromycin on clinical isolates of Mannheimia haemolytica. Am J Vet Res. 2015 Oct;76(10):860-8. doi: 10.2460/ajvr.76.10.860. PMID: 26413823.

6: Moore GM, Basson RP, Tonkinson LV. Clinical field trials with tilmicosin phosphate in feed for the control of naturally acquired pneumonia caused by Actinobacillus pleuropneumoniae and Pasteurella multocida in swine. Am J Vet Res. 1996 Feb;57(2):224-8. PMID: 8633813.

7: Moore GM, Mowrey DH, Tonkinson LV, Lechtenberg KF, Schneider JH. Efficacy dose determination study of tilmicosin phosphate in feed for control of pneumonia caused by Actinobacillus pleuropneumoniae in swine. Am J Vet Res. 1996 Feb;57(2):220-3. PMID: 8633812.

8: Chirase NK, Purdy CW, Avampato JM. Effect of simulated ambient particulate matter exposure on performance, rectal temperature, and leukocytosis of young Spanish goats with or without tilmicosin phosphate. J Anim Sci. 2004 Apr;82(4):1219-26. doi: 10.2527/2004.8241219x. PMID: 15080345.

9: Hoflack G, Maes D, Mateusen B, Verdonck M, de Kruif A. Efficacy of tilmicosin phosphate (Pulmotil premix) in feed for the treatment of a clinical outbreak of Actinobacillus pleuropneumoniae infection in growing-finishing pigs. J Vet Med B Infect Dis Vet Public Health. 2001 Nov;48(9):655-64. doi: 10.1046/j.1439-0450.2001.00492.x. PMID: 11765801.

10: Frank GH, Duff GC. Effects of tilmicosin phosphate, administered prior to transport or at time of arrival, and feeding of chlortetracycline, after arrival in a feedlot, on Mannheimia haemolytica in nasal secretions of transported steers. Am J Vet Res. 2000 Dec;61(12):1479-83. doi: 10.2460/ajvr.2000.61.1479. PMID: 11131584.

11: Han C, Qi CM, Zhao BK, Cao J, Xie SY, Wang SL, Zhou WZ. Hydrogenated castor oil nanoparticles as carriers for the subcutaneous administration of tilmicosin: in vitro and in vivo studies. J Vet Pharmacol Ther. 2009 Apr;32(2):116-23. doi: 10.1111/j.1365-2885.2008.01009.x. PMID: 19290940.

12: Brumbaugh GW, Simpson RB, Edwards JF, Anders DR, Thomson TD. Susceptibility of Mycobacterium avium sbsp paratuberculosis to monensin sodium or tilmicosin phosphate in vitro and resulting infectivity in a murine model. Can J Vet Res. 2004 Jul;68(3):175-81. PMID: 15352541; PMCID: PMC1142136.

13: Galyean ML, Gunter SA, Malcolm-Callis KJ. Effects of arrival medication with tilmicosin phosphate on health and performance of newly received beef cattle. J Anim Sci. 1995 May;73(5):1219-26. doi: 10.2527/1995.7351219x. PMID: 7665351.

14: Reuter RR, Carroll JA, Dailey JW, Cook BJ, Galyean ML. Effects of dietary energy source and level and injection of tilmicosin phosphate on immune function in lipopolysaccharide-challenged beef steers. J Anim Sci. 2008 Aug;86(8):1963-76. doi: 10.2527/jas.2007-0838. Epub 2008 Apr 11. PMID: 18407986.

15: Duff GC, Walker DA, Malcolm-Callis KJ, Wiseman MW, Hallford DM. Effects of preshipping vs. arrival medication with tilmicosin phosphate and feeding chlortetracycline on health and performance of newly received beef cattle. J Anim Sci. 2000 Feb;78(2):267-74. doi: 10.2527/2000.782267x. PMID: 10709916.

16: Brown SA, Deleeuw NR, Stahl GL, Roof RD. Characterization of plasma and lung concentrations after ceftiofur sodium and tilmicosin phosphate administered subcutaneously to mice. J Vet Pharmacol Ther. 1995 Oct;18(5):385-7. doi: 10.1111/j.1365-2885.1995.tb00610.x. PMID: 8587160.

17: Dingwell RT, Duffield TF, Leslie KE, Keefe GP, DesCoteaux L, Kelton DF, Lissemore KD, Schukken YH, Dick P, Bagg R. The efficacy of intramammary tilmicosin at drying-off, and other risk factors for the prevention of new intramammary infections during the dry period. J Dairy Sci. 2002 Dec;85(12):3250-9. doi: 10.3168/jds.S0022-0302(02)74413-5. PMID: 12512598.

18: Readnour RS, Helton-Groce SL, Dixon SS. Determination of tilmicosin in swine feeds by liquid chromatography. J AOAC Int. 1997 Nov-Dec;80(6):1161-70. PMID: 9419854.

19: Mateusen B, Maes D, Hoflack G, Verdonck M, de Kruif A. A comparative study of the preventive use of tilmicosin phosphate (Pulmotil premix) and Mycoplasma hyopneumoniae vaccination in a pig herd with chronic respiratory disease. J Vet Med B Infect Dis Vet Public Health. 2001 Dec;48(10):733-41. doi: 10.1046/j.1439-0450.2001.00503.x. PMID: 11846018.

20: Von Essen S, Spencer J, Hass B, List P, Seifert SA. Unintentional human exposure to tilmicosin (Micotil 300). J Toxicol Clin Toxicol. 2003;41(3):229-33. doi: 10.1081/clt-120021103. PMID: 12807303.