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PKG drug G1 

Cat. No.: HY-112197 Purity: 99.92%
Handling Instructions

PKG drug G1 targets C42 of PKG Iα. PKG drug 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg USD 820 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

PKG Iα[1]

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].

Molecular Weight

257.31

Formula

C₁₃H₁₁N₃OS

CAS No.

374703-78-3

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
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 103 mg/mL (400.30 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.3886 mL 1.9432 mL 3.8864 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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PKG drug G1
Cat. No.:
HY-112197
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