2. Stem Cell/Wnt
  3. PKG
  4. PKG drug G1

PKG agent G1 targets C42 of PKG Iα. PKG agent G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

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

PKG drug G1 Chemical Structure

PKG drug G1 Chemical Structure

CAS No. : 374703-78-3

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

PKG drug G1 Related Antibodies

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  • Purity & Documentation

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Description

PKG agent G1 targets C42 of PKG Iα. PKG agent G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

IC50 & Target

PKG Iα[1]
Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
14 μM
Compound: 8
Inhibitory activity against CDK4 using recombinant human cyclin D2-CDK4 complex expressed in sf9 cells
Inhibitory activity against CDK4 using recombinant human cyclin D2-CDK4 complex expressed in sf9 cells
[PMID: 11741479]
In Vivo

PKG drug G1 induces vasodilation of isolated resistance blood vessels and blood pressure lowering in a mouse model of angiotensin II–induced hypertension. PKG drug G1 efficiently relaxes WT but not knockin (KI) vessels, which is then assessed in a murine model of hypertension. PKG drug G1 lowers blood pressure in hypertensive WT, but not KI, mice in vivo. PKG drug G1 is tested in vivo in healthy mice implanted with telemetric devices that allow blood pressure and heart rate to be constantly monitored. PKG drug G1 or vehicle control is administrated by intraperitoneal injection, and the acute impact on hemodynamics assessed. PKG drug G1 administered at 7.4 mg/kg does not decrease blood pressure, but there is a concomitant reflex tachycardia. When this is repeated using 14.8 mg/kg dose of PKG drug G1, again blood pressure is not altered-but this higher dose induces a potentiated increase in heart rate[1].

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

257.31

Formula

C13H11N3OS
CAS No.
Appearance

Solid

Color

Light brown to reddish brown

SMILES

O=C(/C(N1)=C/C2=C(C)NC3=C2C=CC=C3)NC1=S
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (291.48 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 3.8864 mL 19.4318 mL 38.8636 mL
5 mM 0.7773 mL 3.8864 mL 7.7727 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

Mice[1]
Mice constitutively expressing PKG Iα Cys42Ser are generated on a pure C57BL/6 background. Age-matched and body weight–matched WT or PKG Iα Cys42Ser KI male mice are used in all studies. Blood pressure and heart rate are assessed by radio telemetry in conscious freely moving mice. Alzet osmotic mini-pumps are used to deliver angiotensin II at 1.1 mg/kg per day in some studies. PKG drug G1 is delivered intraperitoneally (3.7-14.8 mg/kg) or orally (20 mg/kg) in some studies. To deliver PKG drug G1 orally, without stress or risk of dislodging the telemetric probe catheter, it is provided suspended in water and set in gelatin flavored with sodium saccharin[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8864 mL 19.4318 mL 38.8636 mL 97.1591 mL
5 mM 0.7773 mL 3.8864 mL 7.7727 mL 19.4318 mL
10 mM 0.3886 mL 1.9432 mL 3.8864 mL 9.7159 mL
15 mM 0.2591 mL 1.2955 mL 2.5909 mL 6.4773 mL
20 mM 0.1943 mL 0.9716 mL 1.9432 mL 4.8580 mL
25 mM 0.1555 mL 0.7773 mL 1.5545 mL 3.8864 mL
30 mM 0.1295 mL 0.6477 mL 1.2955 mL 3.2386 mL
40 mM 0.0972 mL 0.4858 mL 0.9716 mL 2.4290 mL
50 mM 0.0777 mL 0.3886 mL 0.7773 mL 1.9432 mL
60 mM 0.0648 mL 0.3239 mL 0.6477 mL 1.6193 mL
80 mM 0.0486 mL 0.2429 mL 0.4858 mL 1.2145 mL
100 mM 0.0389 mL 0.1943 mL 0.3886 mL 0.9716 mL
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PKG drug G1 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:

PKG drug G1374703-78-3PKG drug G 1PKG drug G-1PKGInhibitorinhibitorinhibit

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