A nonpeptide agonist of PKR1 and PAM of PKR2
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IS20

Item No. 45324

Technical Information
Formal Name
N-[(1Z)-2-(4-methoxyphenyl)-1-[[(3-pyridinylmethyl)amino]carbonyl]ethenyl]-benzamide
CAS Number
1322013-92-2
Molecular Formula
C23H21N3O3
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
COC(C=C1)=CC=C1/C=C(C(NCC2=CN=CC=C2)=O)\NC(C3=CC=CC=C3)=O
InChi Code
InChI=1S/C23H21N3O3/c1-29-20-11-9-17(10-12-20)14-21(26-22(27)19-7-3-2-4-8-19)23(28)25-16-18-6-5-13-24-15-18/h2-15H,16H2,1H3,(H,25,28)(H,26,27)/b21-14-
InChi Key
KKDANILRTKQMGA-STZFKDTASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    IS20 is a nonpeptide agonist of prokineticin receptor 1 (PKR1) and a positive allosteric modulator (PAM) of PKR2.1 It increases intracellular calcium release and Akt phosphorylation in PKR1-expressing CHO cells (EC50 = 44 nM). It also enhances prokineticin-induced ERK phosphorylation in PKR2-expressing CHO cells when used at a concentration of 1 nM. IS20 (0.5 mg/kg, i.p.) increases survival, reduces cardiac lesion formation, improves cardiac function, and increases neovasculogenesis in a mouse model of myocardial infarction.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gasser, A., Brogi, S., Urayama, K., et al. Discovery and cardioprotective effects of the first non-peptide agonists of the G protein-coupled prokineticin receptor-1. PLoS One 10(4), e0121027 (2015).