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Cat. No.: HY-151203

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PKG1α activator 3

PKG1α activator 3 is a PKG1α activator (EC₅₀ basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research.

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

CAS No.: 2773367-58-9
Formula: C₂₇H₂₆Cl₂N₂O₆
Molecular Weight:545.41

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

PKG1α activator 3 Chemical Structure

CAS No.: 2773367-58-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

In Vitro

PKG1α activator 3 (11.7-33.3 μM; 45 min) shows phosphorylation of VASP^[1].
PKG1α activator 3 (6.2-22.8 μM; 24 h) inhibits PDGF-induced cell proliferation^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Smooth muscle cells
Concentration:

6.2-22.8 μM
Incubation Time:

24 hours
Result:

Inhibited hPASMC proliferation EC₅₀ value of 6 μM.

Cell Viability Assay^[1]

Cell Line:

HEK 293 cells
Concentration:

11.7-33.3 μM
Incubation Time:

45 min
Result:

Showed pVASP cell EC₅₀ value of 13.4 μM.

In Vivo

PKG1α activator 3 shows acceptable in vivo rat pharmacokinetic profiles^[1].

		pharmacokinetic parameters
Compound	Cl (mL/min/kg)	Vd (L/kg)	MRT (h)	PPB (%)
PKG1α activator 3	8.1	0.45	0.9	>99.9

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

Related Protocols :

Chemical Information

CAS No. 2773367-58-9
Molecular Weight 545.41
Formula C₂₇H₂₆Cl₂N₂O₆
SMILES

O=C(O)C1=CC=C(CN2[C@@H](C3=CC=CC=C3)[C@@H](O[C@@H](C4=CC(Cl)=CC(Cl)=C4)CO)CCC2)C([N+]([O-])=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Victor W Mak, et al. Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α. J Med Chem. 2022 Aug 11;65(15):10318-10340. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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