A PKGIα activator
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PKG Drug G1

Item No. 29768

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(2-methyl-1H-indol-3-yl)methylene]-2-thioxo-4-imidazolidinone
CAS Number
374703-78-3
Molecular Formula
C13H11N3OS
Formula Weight
257.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): Partially soluble
λmax
228, 286, 415 nm
SMILES
CC1=C(/C=C2C(NC(N/2)=S)=O)C3=CC=CC=C3N1
InChi Code
InChI=1S/C13H11N3OS/c1-7-9(6-11-12(17)16-13(18)15-11)8-4-2-3-5-10(8)14-7/h2-6,14H,1H3,(H2,15,16,17,18)/b11-6-
InChi Key
SNLLEQAPNVMOOT-WDZFZDKYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $36

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    10 mg

    $63

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    50 mg

    $268

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    100 mg

    $469

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    Product Description

    PKG drug G1 is an activator of protein kinase GIα (PKGIα).1 It induces relaxation in U-46619-precontracted mesenteric arteries isolated from wild-type, but not oxidation-insensitive Cys42Ser PKGIα knock-in, mice in a concentration-dependent manner. PKG drug G1 (14.8 mg/kg) induces oxidation of PKGIα, a marker of activation, in the aorta in a mouse model of angiotensin II-induced hypertension. It decreases mean arterial pressure in the same model when administered at a dose of 20 mg/kg per day for four days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burgoyne, J.R., Prysyazhna, O., Richards, D.A., et al. Proof of principle for a novel class of antihypertensives that target the oxidative activation of PKG Iα (protein kinase G Iα). Hypertension 70(3), 577-586 (2017).