MY-5445

MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.

Product information

CAS Number: 78351-75-4

Molecular Weight: 331.80

Formula: C20H14ClN3

Chemical Name: N-(3-chlorophenyl)-4-phenylphthalazin-1-amine

Smiles: ClC1=CC(=CC=C1)NC1=NN=C(C2C=CC=CC=21)C1C=CC=CC=1

InChiKey: CEHQLKSLMFIHBF-UHFFFAOYSA-N

InChi: InChI=1S/C20H14ClN3/c21-15-9-6-10-16(13-15)22-20-18-12-5-4-11-17(18)19(23-24-20)14-7-2-1-3-8-14/h1-13H,(H,22,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (150.69 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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 . MY-5445 selectively reverses ABCG2-mediated multidrug resistance in ABCG2-overexpressing cells. MY-5445 reverses ABCG2-mediated multidrug resistance (MDR) by potentiating the cytotoxicity of an ABCG2 substrate drug in ABCG2-overexpressing multidrug-resistant cancer cells, possibly by modulating the function and/or the protein expression of ABCG2. MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis in S1-M1-80 cell.

In Vivo:

MY-5445 (0.5-3 mg/kg; i.p.; twice a day; for 15 days) produces a significant relief of mechanical hypersensitivity.

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.

Products are for research use only. Not for human use.