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Purity: ≥98%
MY-5445 is a potent inhibitor of platelet aggregatio. The concentrations of MY-5445 producing 50% inhibition of human platelet aggregation induced by 3 microM ADP, 3 micrograms/ml of collagen and 100 micrograms/ml of arachidonic acid were 0.07, 0.02 and 0.17 microM, respectively. Addition of MY-5445 significantly elevated cyclic GMP content in human platelets but had no effect on cyclic AMP content, suggesting that the drug affects principally the cyclic GMP metabolism in the platelet. Although MY-5445 had no effect on either adenylate cyclase or guanylate cyclase activity, it inhibited specifically human platelet cyclic GMP phosphodiesterase which was separated from cyclic AMP phosphodiesterase by diethylaminoethyl-cellulose column chromatography. The inhibitory effect of MY-5445 on cyclic GMP phosphodiesterase was also demonstrated by direct binding of the enzyme to MY-5445 coupled Sepharose, which was a useful tool for purifying the cyclic GMP phosphodiesterase from human platelet. These results would suggest that MY-5445 inhibits human platelet aggregation by increasing cyclic GMP content and that it provides a useful probe for elucidating the role of cyclic GMP in platelet aggregation.
| ln Vitro |
By raising the level of cyclic GMP, MY-5445 prevents human platelet aggregation and serves as a helpful probe to clarify the function of cyclic GMP in platelet aggregation [1]. MY-5445 specifically reverses multidrug resistance mediated by ABCG2 in cells that overexpress ABCG2 [2]. By controlling ABCG2 functionand/or protein expression, MY-5445 may improve the cytotoxicity of ABCG2 substrate medications in ABCG2-overexpressing multidrug-resistant cancer cells, thereby reversing ABCG2-mediated multidrug resistance (MDR) [2]. Topotecan-induced apoptosis in S1-M1-80 cells is significantly increased by MY-5445 (3 μM; 48 hours) [2].
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| ln Vivo |
Mechanical hypersensitivity is considerably reduced by MY-5445 (0.5–3 mg/kg; intraperitoneal injection; twice daily; for 15 days) [3].
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| Cell Assay |
Apoptosis analysis [2]
Cell Types: human S1 colon cancer cells, S1-M1-80 cancer cells Tested Concentrations: 3 μM Incubation Duration: 48 hrs (hours) Experimental Results: Drug-induced apoptosis is enhanced in ABCG2 overexpressing cancer cells. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J male mice [3]
Doses: 0.5 mg/kg, 3 mg/kg Route of Administration: intraperitoneal (ip) injection, twice a day for 15 days. Experimental Results: Allodynia caused by the cuff was diminished. |
| References |
[1]. Souness JE, et al. Role of selective cyclic GMP phosphodiesterase inhibition in the myorelaxant actions of M&B 22,948, MY-5445, vinpocetine and 1-methyl-3-isobutyl-8-(methylamino)xanthine. Br J Pharmacol. 1989 Nov;98(3):725-34.
[2]. Chung-Pu Wu, et al. MY-5445, a phosphodiesterase type 5 inhibitor, resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic anticancer drugs. Am J Cancer Res. 2020; 10(1): 164-178. [3]. Maud Bollenbach, et al. Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model. Eur J Med Chem. 2019 Sep 1;177:269-290. |
| Molecular Formula |
C20H14CLN3
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| Molecular Weight |
331.80
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| CAS # |
78351-75-4
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| SMILES |
ClC1=CC(NC2=NN=C(C3=CC=CC=C3)C4=C2C=CC=C4)=CC=C1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| 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 (7.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0139 mL | 15.0693 mL | 30.1386 mL | |
| 5 mM | 0.6028 mL | 3.0139 mL | 6.0277 mL | |
| 10 mM | 0.3014 mL | 1.5069 mL | 3.0139 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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