| Size | Price | Stock | Qty |
|---|---|---|---|
| 500μg |
|
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| 1mg | |||
| Other Sizes |
| Targets |
HCV[1]; Bacterial[2]; Parasite[3]
Bacterial ribosomes (protein synthesis), HCV entry, and Plasmodium falciparum. Micrococcin P1 functions by inhibiting protein synthesis through binding to bacterial ribosomes and preventing polypeptide elongation. It inhibits HCV entry in a pan-genotypic manner. |
|---|---|
| ln Vitro |
Micrococcin P1 is extremely powerful, with a minimum inhibitory concentration (MIC) of 32–63 nM, according to dose-response studies. Cytotoxicity studies on the hepatic cell line HepG2 and the monocytic cell line THP-1 over a 40-hour period showed no discernible effect on cell line growth (<10% inhibition at 30 mM), resulting in a selectivity index larger than 500. examines Micrococcin P1's intracellular activities as well; it functions against M that expresses GFP. H37Rv TB developing inside RAW 264.7 macrophages, showing a potency similar to isoniazid at an IC80 of roughly 1 mM[1].
Micrococcin P1 is a potent HCV inhibitor with an EC₅0 range of 0.1-0.5 microM. It has in vitro antibacterial activity against Gram-positive strains with MICs of 2 microg/mL (S. aureus), 1 microg/mL (E. faecalis), and 1 microg/mL (S. pyogenes). Dose-response assays revealed a MIC of 32-63 nM. It is active against GFP-expressing M. tuberculosis H37Rv inside RAW 264.7 macrophages with an IC₅0 of about 1 mM. Cytotoxicity assays showed no significant impairment on HepG2 or THP-1 cell line growth (<10% inhibition at 30 mM) over 40 hours, yielding a selectivity index >500. |
| ln Vivo |
No detailed in vivo activity data has been reported for Micrococcin P1. As a macrocyclic peptide antibiotic with antiviral and antiparasitic activities, it could potentially be evaluated in animal models of bacterial, viral, or parasitic infections.
|
| Enzyme Assay |
HCV entry inhibition assays: Micrococcin P1 is tested in HCV cell culture systems. Antibacterial activity is assessed using broth microdilution assays against Gram-positive bacterial strains. Antimalarial activity is evaluated against P. falciparum cultures. MIC and EC₅0 values are calculated from dose-response curves.
|
| Cell Assay |
Antibacterial activity is evaluated using standard broth microdilution assays against Gram-positive bacterial strains. MICs are determined after incubation. Antiviral activity against HCV is assessed in cell culture systems. Cytotoxicity is evaluated in HepG2 and THP-1 cells using MTT or CellTiter-Glo assays. Intracellular activity against M. tuberculosis is assessed in infected RAW 264.7 macrophages.
|
| Animal Protocol |
Animal models of bacterial infection (e.g., murine models of S. aureus infection) or HCV infection could be used to evaluate Micrococcin P1 in vivo. Efficacy would be assessed by bacterial load reduction, viral load, and survival.
|
| ADME/Pharmacokinetics |
Micrococcin P1 has a molecular weight of 1144.37 and a molecular formula of C4₈H4₉N13O₉S₆. It is a macrocyclic peptide antibiotic. Storage: powder at -20degC for 3 years; in solvent at -80degC for 6 months.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for Micrococcin P1. Cytotoxicity assays showed no significant impairment on HepG2 or THP-1 cell growth (<10% inhibition at 30 mM) over 40 hours. As a research compound, it is not intended for human therapeutic use.
|
| References |
|
| Additional Infomation |
13',19'-disehydro-19'-deoxy-28,44-dihydro-44-hydroxymicrococcin P has been reported in Bacillus pumilus, and relevant data are available.
See also: Micrococcin (note moved to). Micrococcin P1 is a macrocyclic peptide antibiotic that inhibits HCV entry (EC₅0 0.1-0.5 microM), has antibacterial activity against Gram-positive bacteria, and inhibits P. falciparum. The compound is for research use only and has not entered clinical trials. |
| Molecular Formula |
C48H49N13O9S6
|
|---|---|
| Molecular Weight |
1144.37
|
| Exact Mass |
1143.21
|
| CAS # |
67401-56-3
|
| PubChem CID |
91755078
|
| Appearance |
White to yellow solid powder
|
| LogP |
7.665
|
| Hydrogen Bond Donor Count |
9
|
| Hydrogen Bond Acceptor Count |
22
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
76
|
| Complexity |
2180
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
C/C=C\1/C2=NC(=CS2)C(=O)N[C@H](C3=NC(=CS3)C(=O)N[C@H](C4=NC(=CS4)C5=C(C=CC(=N5)C6=NC(=CS6)C7=NC(=CS7)C(=O)N/C(=C\C)/C(=O)NC[C@@H](C)O)C8=NC(=CS8)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)[C@@H](C)O)C(C)C
|
| InChi Key |
MQGFYNRGFWXAKA-QMXXNAFJSA-N
|
| InChi Code |
InChI=1S/C48H49N13O9S6/c1-8-24(37(65)49-12-20(5)62)51-38(66)28-15-73-46(56-28)32-18-74-45(58-32)26-11-10-23-36(50-26)27-13-75-48(53-27)35(22(7)64)61-41(69)31-17-76-47(57-31)33(19(3)4)59-39(67)30-16-72-44(55-30)25(9-2)52-42(70)34(21(6)63)60-40(68)29-14-71-43(23)54-29/h8-11,13-22,33-35,62-64H,12H2,1-7H3,(H,49,65)(H,51,66)(H,52,70)(H,59,67)(H,60,68)(H,61,69)/b24-8-,25-9-/t20-,21-,22-,33+,34+,35+/m1/s1
|
| Chemical Name |
2-[2-[(12S,19S,26Z,29S)-26-ethylidene-12,29-bis[(1R)-1-hydroxyethyl]-14,21,28,31-tetraoxo-19-propan-2-yl-10,17,24,34-tetrathia-6,13,20,27,30,35,36,37,38-nonazahexacyclo[30.2.1.18,11.115,18.122,25.02,7]octatriaconta-1(35),2(7),3,5,8,11(38),15,18(37),22,25(36),32-undecaen-5-yl]-1,3-thiazol-4-yl]-N-[(Z)-1-[[(2R)-2-hydroxypropyl]amino]-1-oxobut-2-en-2-yl]-1,3-thiazole-4-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8738 mL | 4.3692 mL | 8.7384 mL | |
| 5 mM | 0.1748 mL | 0.8738 mL | 1.7477 mL | |
| 10 mM | 0.0874 mL | 0.4369 mL | 0.8738 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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