| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
OVCAR-3, SKOV-3, and A2780 are ovarian cancer cell lines whose proliferation and clonal activity are inhibited by minocycline (0-100 μM, 24-72 hours) [3]. Minocycline (0-100 μM, 24-48 hours) inhibits DNA incorporation and cyclins, which stops the cell cycle [3]. Ovarian cancer cell lines undergo apoptosis when exposed to minocycline (0-100 μM) for 72 hours [3]. Minocycline inhibits both caspase-dependent and caspase-independent cell death after exhibiting direct neuronal protection, a mechanism of protection that may be connected to the maintenance of mitochondrial integrity and cytochrome c [2]. Hypoxia-inducible factor (HIF)-1α is inhibited by minocycline, which also increases p53 protein levels and deactivates the AKT/mTOR/p70S6K/4E-BP1 pathway [6].
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| ln Vivo |
In female nude mice, minocycline (0–30 mg/kg) taken orally once a day for four weeks inhibits the growth of OVCAR-3 tumors [3]. When given at large intraperitoneal doses, minocycline (IP) is a neuroprotective agent in animal models of cerebral ischemia [1]. Mice exposed to a single intraperitoneal injection of minocycline (0–40 mg/kg) can greatly reduce the development of behavioral sensitization and excessive movement brought on by METH [2]. The temporary middle cerebral artery occlusion model (TMCAO) can effectively reduce infarct size when administered intravenously with 3 or 10 mg/kg of minocycline once [1]. Serum levels (3 mg/kg) of minocycline (3–10 mg/kg IV, once) are comparable to those attained following the typical 200 mg dose in humans [1]. Rats' ischemia-induced ventricular arrhythmias are lessened by minocycline. The activation of the L-type Ca2+ channel, mitochondrial KATP channel, and PI3K/Akt signaling pathway may be connected to this effect [7].
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| Cell Assay |
Cell proliferation assay[3]
Cell Types: Human ovarian cancer cell lines (OVCAR-3, SKOV-3 and A2780) and primary cells (HEK-293, HMEC, HUVEC, ATCC) Tested Concentrations: 0, 1, 10, 50 and 100 μM Incubation Duration: 24, 48 or 72 h Experimental Results: Inhibited the proliferation of OVCAR-3, SKOV-3 and A2780 cells in a concentration-dependent manner, with IC50 values of 62.0, 56.1 and 59.5 μM respectively. There was no effect on the viability of HEK-293 or HUVEC. Cell cycle analysis[3] Cell Types: OVCAR-3, SKOV-3 and A2780 Cell Tested Concentrations: 0, 10, 50 and 100 μM Incubation Duration: 24 or 48 hrs (hours) Experimental Results: G0-G1 phase cells were Block in a time-dependent manner. At 100 μM, the percentage of cells in S phase and G2-M phase diminished by more than 80%. Western Blot Analysis[3] Cell Types: OVCAR-3, SKOV-3 and A2780 Cell Tested Concentrations: 0, 10, 50 and 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cyclins A, B and E were expressed at low levels. caspase- increasing by 3 levels increased more than 3.0-fold at 100 μM. Minocy |
| Animal Protocol |
Animal/Disease Models: Female nude mice (6 weeks old, 9 mice per group, each mouse was injected with OVCAR-3 cells subcutaneously (sc) (sc) on the left side of the abdomen) [3]
Doses: 10 or 30 mg/kg Route of Administration: Oral administration through drinking water The drug was administered one time/day starting on the 8th day of cell inoculation for 4 weeks. Experimental Results: Inhibited the growth of OVCAR-3 tumors in these female nude mice and diminished microvessel density. Animal/Disease Models: Male Balb/cAnNCrICrIj mice (8 weeks old, 23-30 g, methamphetamine (METH, 3 mg/kg) subcutaneously (sc) (sc) (sc) in a volume of 10 ml/kg) [2] Doses: 0, 10 , 20 or 40 mg/kg Route of Administration: intraperitoneal (ip) injection, once, 30 minutes before METH administration Experimental Results: At the 40 mg/kg dose, the development of METH-induced hyperlocomotion and behavioral hypersensitivity was Dramatically attenuated in mice. It had no effect on the induction of METH-induced hyperthermia in mice. Dramatically attenuated reductions in DA and DOPAC in the striatum. S |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Many reviews state that tetracyclines are contraindicated during breastfeeding because of possible staining of infants' dental enamel or bone deposition of tetracyclines. However, a close examination of available literature indicates that there is not likely to be harm in short-term use of minocycline during lactation because milk levels are low and absorption by the infant is inhibited by the calcium in breastmilk. Short-term use of minocycline is acceptable in nursing mothers. As a theoretical precaution, avoid prolonged or repeat courses during nursing. Monitor the infant for rash and for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis (thrush, diaper rash). Black discoloration of breastmilk has been reported with minocycline. Topical minocycline for acne by the mother poses no risk to the breastfed infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk A woman taking minocycline 100 mg twice daily for almost 4 years developed galactorrhea after taking perphenazine, amitriptyline and diphenhydramine, and the breast secretion was black in color. Another woman who had nursed her infant and produced occasional small amounts of breastmilk during the 18 months after weaning was given oral minocycline 150 mg daily. After 3 to 4 weeks, expressed milk had become black. Iron levels in milk were over 100 times greater than that found in normal milk. A mammogram was normal. In both of these cases, macrophages containing a black, iron-containing pigment were found in milk. It is thought that the pigment is an iron chelate of minocycline or one of its metabolites. |
| References |
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| Additional Infomation |
Minocycline is a tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5. It has a role as an antibacterial drug, an Escherichia coli metabolite and a geroprotector. It is a member of tetracyclines, a tetracenomycin and a tertiary alpha-hydroxy ketone. It is a conjugate acid of a minocycline(1-). It is a tautomer of a minocycline zwitterion.
Minocycline is a Tetracycline-class Drug. The physiologic effect of minocycline is by means of Decreased Prothrombin Activity. A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections. See also: Minocycline (annotation moved to). |
| Molecular Formula |
C23H27N3O7
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|---|---|
| Molecular Weight |
457.48
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| Exact Mass |
457.184
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| CAS # |
10118-90-8
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| Related CAS # |
Minocycline hydrochloride;13614-98-7;Minocycline-d6;1036070-10-6
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| PubChem CID |
54675783
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
803.3±65.0 °C at 760 mmHg
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| Flash Point |
439.6±34.3 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.718
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| LogP |
-0.65
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
33
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| Complexity |
971
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
CN(C1=CC=C(O)C2=C1C[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C([C@@]4(O)C(O)=C3C2=O)=O)C
|
| InChi Key |
FFTVPQUHLQBXQZ-KVUCHLLUSA-N
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| InChi Code |
InChI=1S/C23H27N3O7/c1-25(2)12-5-6-13(27)15-10(12)7-9-8-11-17(26(3)4)19(29)16(22(24)32)21(31)23(11,33)20(30)14(9)18(15)28/h5-6,9,11,17,27-28,31,33H,7-8H2,1-4H3,(H2,24,32)/t9-,11-,17-,23-/m0/s1
|
| Chemical Name |
(4S,4aS,5aR,12aR)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide
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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) |
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
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|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1859 mL | 10.9294 mL | 21.8589 mL | |
| 5 mM | 0.4372 mL | 2.1859 mL | 4.3718 mL | |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1859 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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