Lymecycline is a broad-spectrum antibacterial drug derived from tetracycline that disrupts the ribosomal production of prokaryotic proteins. Anti-inflammatory properties are also shown in memecycline [1].

Absorption, Distribution and Excretion
Following oral administration, lymecycline is absorbed in 77-88% of its solution, with a relative bioavailability of 70%. The peak plasma concentration (Cmax) of lymecycline is 2.1 mg/L, reached approximately 3 hours after administration. The AUC is 21.9 ± 4.3 mg·h/L. Approximately 25% of lymecycline is excreted in the urine. As it is a tetracycline, fecal excretion is likely another route of excretion. Limecycline is lipophilic, readily crosses cell membranes, and passively diffuses through bacterial porin channels. As a second-generation tetracycline, its concentration in bile is 10 to 25 times higher than its plasma concentration. Generally, the volume of distribution for tetracyclines is 1.3–1.7 L/kg or 100–130 L. Like other tetracyclines, lymecycline is partially cleared by the kidneys.

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Biological Half-Life
The half-life of lymecycline is approximately 8 hours.

[1]. Rempe S, et al. Tetracyclines and pulmonary inflammation. Endocr Metab Immune Disord Drug Targets. 2007 Dec;7(4):232-6.

Limecycline is a broad-spectrum tetracycline-based antibiotic. Its solubility is approximately 5000 times that of tetracycline bases, and unlike other tetracycline antibiotics, it can be absorbed through active transport via the intestinal wall. Limecycline possesses a variety of antibacterial activities, including protein synthesis inhibitor, antigenic animal drug, antibacterial agent, and antimicrobial agent. It belongs to the tetracycline class of antibiotics and is also a tertiary α-hydroxy ketone. Limecycline is a broad-spectrum second-generation tetracycline antibiotic used to treat acne and other infections caused by susceptible bacteria. It has proven to be a cost-effective alternative to minocycline, with comparable safety and efficacy. Limecycline was first discovered in 1961. It is manufactured by Galderma and used in the UK, New Zealand, and other countries. Limecycline is not marketed in the US, but equivalent drugs such as minocycline and tetracycline are available. Limecycline is a semi-synthetic tetracycline-related antibiotic. It is more readily absorbed than tetracycline and can be used at lower doses. Drug Indications Limecycline is used to treat acne and other infections caused by susceptible bacteria; Propionibacterium acnes is commonly the pathogen of acne. Infections that lismecycline can treat include upper respiratory tract infections, urinary tract infections, bronchitis, chlamydia infections, and rickettsial infections. Mechanism of Action Normally, ribosomes synthesize proteins by binding aminoacyl-tRNA to the mRNA-ribosome complex. Limecycline binds to the 30S ribosomal subunit, preventing aminoacyl-tRNA from binding to the A site of the ribosome, thereby preventing polypeptide chain elongation. This results in its antibacterial activity, making it suitable for treating a variety of infections. Pharmacodynamics Like other tetracyclines, lismecycline has antibacterial activity against both intracellular and extracellular bacteria and can be used to treat infections caused by susceptible bacteria. Studies have shown that lismecycline is safe and effective in treating moderate to severe acne. It is worth noting that, like other tetracyclines, lismecycline may cause esophageal irritation and ulcers, which can be prevented by drinking plenty of water during treatment. It may also cause photosensitivity. Limecycline can cause renal tubular acidosis or hepatotoxicity. This medication is not recommended for patients with kidney disease or severe liver disease.

C29H38N4O10

602.641

602.259

992-21-2

Lymecycline-d8

54707177

Typically exists as solid at room temperature

1.53

840.5ºC at 760 mmHg

192.5°C

462.1ºC

1.693

1.027

9

13

10

43

1230

6

OC([C@H](CCCCNCNC(C1=C(O)[C@@H](N(C)C)[C@@]2(C[C@@]3([C@@](O)(C)C4=CC=CC(O)=C4C(=O)C3=C(O)[C@]2(O)C1=O)[H])[H])=O)N)=O

PZTCVADFMACKLU-UEPZRUIBSA-N

InChI=1S/C29H38N4O10/c1-28(42)13-7-6-9-17(34)18(13)22(35)19-14(28)11-15-21(33(2)3)23(36)20(25(38)29(15,43)24(19)37)26(39)32-12-31-10-5-4-8-16(30)27(40)41/h6-7,9,14-16,21,31,34-35,38,42-43H,4-5,8,10-12,30H2,1-3H3,(H,32,39)(H,40,41)/t14-,15-,16-,21-,28+,29-/m0/s1

(2S)-6-[[[(4S,4aS,5aS,6S,12aR)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carbonyl]amino]methylamino]-2-aminohexanoic acid

Tetralisal Mucomycin Lymecycline

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

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)