| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
MK-447 (MK447) is a novel and potent free radical scavenger. In addition, it functions as a nonsteroidal anti-inflammatory drug (NSAID-like) and promotes the synthesis of PGH2, endoperoxide, and other prostaglandins.
| Targets |
PGI2
MK-447 is a free radical scavenger that decreases endoperoxide accumulation (PGG2) and increases endoperoxide formation (PGH2) as well as the formation of other prostaglandins[1]. MK-447 (100 μM) raises prostaglandin I2 (PGI2) levels. In the isolated rat aorta, MK-447 also speeds up endogenous PGI2 production[2]. |
|---|---|
| ln Vitro |
MK-447 is a free radical scavenger that decreases endoperoxide accumulation (PGG2) and increases endoperoxide formation (PGH2) as well as the formation of other prostaglandins[1]. MK-447 (100 μM) raises prostaglandin I2 (PGI2) levels. In the isolated rat aorta, MK-447 also speeds up endogenous PGI2 production[2].
MK-447 (at concentrations of 30 and 100 μM) significantly accelerated the generation and release of prostacyclin (PGI2) from endogenous arachidonic acid in isolated, mechanically stimulated rat aortic strips. Compared to the PGI2 level before its addition (set as 100%), MK-447 at 30 μM increased PGI2 generation to 113.8% and at 100 μM increased it to 139.2%. The anti-aggregatory activity in the medium was confirmed to be PGI2 based on its half-life (11-14 min) and inhibition by indomethacin and 15-HPETE. [2] In separate tests, MK-447 (10-100 μM) did not affect rabbit platelet aggregation induced by ADP, arachidonic acid, or collagen, indicating it does not directly interfere with these aggregation pathways or the anti-aggregatory activity of PGI2 itself. [2] |
| ln Vivo |
MK-447 (20 and 50 mg/kg, p.o.) inhibits the production of gastric acid in rats with a 4-hour pylorus ligation, but has no effect on the production of gastric pepsin. MK-447 dose-dependently reduces canine acid output at 5, 10, 20, and 40 mg/kg, p.o.[1].
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| Animal Protocol |
The animal experiment described involves tissue harvesting for ex vivo organ bath studies. Thoracic and abdominal aortae were isolated from male Sprague-Dawley rats (8-10 weeks old). The aortae were cut longitudinally into strips. The protocol does not involve administering MK-447 to live animals for pharmacokinetic or efficacy studies. [2]
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| References | |
| Additional Infomation |
In a previously cited study, MK-447 was referred to as a “basic anti-inflammatory agent.” [2]
The study showed that the mechanism by which MK-447 accelerates PGI2 production in isolated rat aorta is its activity as a tryptophan-like cofactor of prostaglandin hydroperoxidase, which catalyzes the conversion of PGG2 to PGH2, a precursor of PGI2 synthesis. This mechanism is considered to be different from other known PGI2 biosynthetic stimulants. [2] Given that PGI2 is a potent inhibitor of platelet aggregation and is continuously released from endothelial cells, the authors suggest that MK-447 may be a good candidate for preventing thrombosis because it can selectively stimulate PGI2 production in the presence of arachidonic acid. [2] |
| Molecular Formula |
C11H16INO
|
|---|---|
| Molecular Weight |
305.15531539917
|
| Exact Mass |
305.028
|
| CAS # |
58456-91-0
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| PubChem CID |
119286
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.552g/cm3
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| Boiling Point |
306.9ºC at 760mmHg
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| Flash Point |
139.4ºC
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| LogP |
3.453
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
|
| Complexity |
190
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC1=C(I)C=C(C(C)(C)C)C=C1CN
|
| InChi Key |
SSEAPVMQZPKNQZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H16INO/c1-11(2,3)8-4-7(6-13)10(14)9(12)5-8/h4-5,14H,6,13H2,1-3H3
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| Chemical Name |
2-(aminomethyl)-4-tert-butyl-6-iodophenol
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| Synonyms |
MK-447; MK447; MK 447
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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 | 3.2770 mL | 16.3848 mL | 32.7697 mL | |
| 5 mM | 0.6554 mL | 3.2770 mL | 6.5539 mL | |
| 10 mM | 0.3277 mL | 1.6385 mL | 3.2770 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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