2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. MY-5445

MY-5445 est un inhibiteur spécifique de la phosphodiestérase de type 5 (PDE5). MY-5445 inhibe sélectivement PDE cGMP avec un Ki de 1,3 μM.

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.

For research use only. We do not sell to patients.

MY-5445 Chemical Structure

MY-5445 Chemical Structure

CAS No. : 78351-75-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 120 In-stock
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

MY-5445 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1][3]

PDE5

1.3 μM (Ki)

PDE5

6.7 μM (IC50)

PDE4

37 μM (IC50)

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 [1].
MY-5445 selectively reverses ABCG2-mediated multidrug resistance in ABCG2-overexpressing cells[2].
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[2].
MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis in S1-M1-80 cell[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MY-5445 Related Antibodies

Apoptosis Analysis[2]

Cell Line: Human S1 colon cancer cells, S1-M1-80 cancer cells
Concentration: 3 μM
Incubation Time: 48 hours
Result: Enhanced drug-induced apoptosis in ABCG2-overexpressing cancer cells.
In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J male mice[3]
Dosage: 0.5 mg/kg, 3 mg/kg
Administration: Intraperitoneal injection, twice a day, for 15 days
Result: Alleviated the cuff-induced allodynia.
Molecular Weight

331.80

Formula

C20H14ClN3
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

ClC1=CC(NC2=NN=C(C3=CC=CC=C3)C4=C2C=CC=C4)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (150.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.86%

SDS (393 KB)

COA (252 KB) HNMR (280 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0139 mL 15.0693 mL 30.1386 mL 75.3466 mL
5 mM 0.6028 mL 3.0139 mL 6.0277 mL 15.0693 mL
10 mM 0.3014 mL 1.5069 mL 3.0139 mL 7.5347 mL
15 mM 0.2009 mL 1.0046 mL 2.0092 mL 5.0231 mL
20 mM 0.1507 mL 0.7535 mL 1.5069 mL 3.7673 mL
25 mM 0.1206 mL 0.6028 mL 1.2055 mL 3.0139 mL
30 mM 0.1005 mL 0.5023 mL 1.0046 mL 2.5116 mL
40 mM 0.0753 mL 0.3767 mL 0.7535 mL 1.8837 mL
50 mM 0.0603 mL 0.3014 mL 0.6028 mL 1.5069 mL
60 mM 0.0502 mL 0.2512 mL 0.5023 mL 1.2558 mL
80 mM 0.0377 mL 0.1884 mL 0.3767 mL 0.9418 mL
100 mM 0.0301 mL 0.1507 mL 0.3014 mL 0.7535 mL
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MY-5445 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MY-544578351-75-4MY5445MY 5445Phosphodiesterase (PDE)plateletaggregationanticancerneuropathic painneuropathicallodyniaInhibitorinhibitorinhibit

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