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Purity: ≥98%
Sarecycline (formerly known as WC-3035 and P005672; trade name: Seysara) is the first narrow spectrum tetracycline-class antibiotic being developed for acne treatment. In Oct 2018, FDA approved Sarecycline for the treatment of inflammatory lesions of non-nodular moderate to severe acne vulgaris in patients 9 years of age and older. In addition to exhibiting activity against important skin/soft tissue pathogens, sarecycline exhibits targeted antibacterial activity against clinical isolates of Cutibacterium acnes In the current study, sarecycline was 16 to 32-fold less active than broad spectrum tetracyclines-such as minocycline and doxycycline-against aerobic Gram-negative bacilli associated with normal human intestinal microbiome. Also, reduced activity against Escherichia coliwas observed in vivo in a murine septicemia model with PD50 values at >40 mg/kg and 5.72 mg/kg for sarecycline and doxycycline, respectively. Sarecycline was also 4 to 8-fold less active against representative anaerobic bacteria that also comprise normal human intestinal microbiome. Additionally, sarecycline displayed a low propensity for resistance development in C. acnes strains, with spontaneous mutation frequencies of 10-10 at 4 to 8-times the MIC, similar to minocycline and vancomycin. When tested against Gram-positive pathogens with defined tetracycline resistance mechanisms, sarecycline was more active than tetracycline against the tet(K) and tet(M) strains, with MIC ranging from 0.125 to 1.0 ug/mL and 8 ug/mL, respectively, compared with 16 to 64 ug/mL and 64 ug/mL for tetracycline, respectively. However, sarecycline activity in the tet(K) and tet(M) strains were decreased compared to wildtype, which demonstrated MIC ranging from 0.06 to 0.25 ug/mL, though not as pronounced as tetracycline.
| ln Vitro |
MIC values for 55 clinical strains of cosmetic acne on stick culture medium are 0.5~16 µg/ml, 0.5 µg/ml for MIC50, and 4 µg/ml for MIC90 [1]. The drug sarecycline exhibits efficacy against macrolide organisms [1]. The degrading aerobic Gram-null bacteria are not much affected by sarecycline hydrochloride [2].
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| ln Vivo |
In a neutropenic mouse infection paradigm, seromycin hydrochloride (0.33–9 mg/kg; intravenously) has demonstrated strong efficacy against Staphylococcus aureus [1]. The ability of serocycline to inhibit E. aureus (PD50=0.25 mg/kg) in an abdominal systemic infection model in CD-1 mice, but not E. Coli at the maximum concentration (>40 mg/kg). The impact is obscure [6].
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| Animal Protocol |
Animal/Disease Models: Carrageenan-induced footpad edema male Sprague Dawley rat model [6]
Doses: 1 mg/kg, 5 mg/kg. kg; intraperitoneal; injection single dose) Anti-inflammatory in the Sprague Dawley rat model activity[6]. ,10 mg/kg, 25 mg/kg, 50 mg/kg, 75 mg/kg, 100 mg/kg, 150 mg/kg Route of Administration: intraperitoneal (ip) injection; single dose. Before injecting a sterile 1 mg/0.1 mL carrageenan solution into the plantar part of the right hind paw. Experimental Results: Compared to baseline, inflammation was diminished to 55.7% and 53.1% at the 75 mg/kg and 100 mg/kg doses, respectively. Animal/Disease Models: Male Sprague Dawley rat model of carrageenan-induced footpad edema [6] Doses: 0.33, 1, 3 or 9 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: At one dose, thigh bacterial load was diminished 2-log10 is comparable to doxycycline, with ED50 of 8.23 and 8.32 mg/kg respectively. |
| References |
[1]. Zhanel G, et al. Microbiological Profile of Sarecycline, a Novel Targeted Spectrum Tetracycline for the Treatment of Acne Vulgaris. Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01297-18.
[2]. Moore AY, et al. Sarecycline: a narrow spectrum tetracycline for the treatment of moderate-to-severe acne vulgaris. Future Microbiol. 2019 Sep;14(14):1235-1242. [3]. Batool Z, et al. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20530-20537. [4]. Butler MS, et al. Antibiotics in the clinical pipeline in 2013. J Antibiot (Tokyo). 2013 Oct;66(10):571-91. [5]. Bunick CG, et al. Antibacterial Mechanisms and Efficacy of Sarecycline in Animal Models of Infection and Inflammation. Antibiotics (Basel). 2021 Apr 15;10(4):439. |
| Additional Infomation |
Sarecycline is a Tetracycline-class Drug. The mechanism of action of sarecycline is as a P-Glycoprotein Inhibitor.
See also: Sarecycline (annotation moved to); Sarecycline Hydrochloride (annotation moved to). |
| Molecular Formula |
C24H29N3O8
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|---|---|
| Molecular Weight |
487.51
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| Exact Mass |
487.195
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| CAS # |
1035654-66-0
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| Related CAS # |
Sarecycline hydrochloride;1035979-44-2
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| PubChem CID |
54681908
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.106
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CN([C@H]1[C@@H]2C[C@@H]3CC4=C(C(C3=C(O)[C@]2(O)C(C(C(N)=O)=C1O)=O)=O)C(O)=CC=C4CN(OC)C)C
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| InChi Key |
AYUMVPHUMFKFPJ-SBAJWEJLSA-N
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| InChi Code |
InChI=1S/C24H29N3O8/c1-26(2)18-13-8-11-7-12-10(9-27(3)35-4)5-6-14(28)16(12)19(29)15(11)21(31)24(13,34)22(32)17(20(18)30)23(25)33/h5-6,11,13,18,28-29,32,34H,7-9H2,1-4H3,(H2,25,33)/t11-,13-,18-,24-/m0/s1
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| Chemical Name |
(4S,4aS,5aR,12aS)-4-(dimethylamino)-3,10,12,12a-tetrahydroxy-7-((methoxy(methyl)amino)methyl)-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
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| Synonyms |
WC-3035; WC 3035; WC3035; P005672; P-005672; P 005672; P005672; trade name: Seysara
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0512 mL | 10.2562 mL | 20.5124 mL | |
| 5 mM | 0.4102 mL | 2.0512 mL | 4.1025 mL | |
| 10 mM | 0.2051 mL | 1.0256 mL | 2.0512 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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