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NH2-c[X-R-L-S-X]-K-G-P- (D-1Nal)

Selected Variant

HY-P3346

Size: 1 Each

NH2-c[X-R-L-S-X]-K-G-P- (D-1Nal) (compound 39) is a potent APJ agonist, with a Ki of 0.6 nM. NH2-c[X-R-L-S-X]-K-G-P- (D-1Nal) can activate Gαi1 (EC50=0.8 nM) and recruit β-arrestin2 (EC50=31 nM) . NH2-c[X-R-L-S-X]-K-G-P- (D-1Nal) exhibits prolonged cardiac effects[1].

Product Specifications

CAS Number

2891469-80-8

UNSPSC

12352005

Target

Apelin Receptor (APJ)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/nh2-c-x-r-l-s-x-k-g-p-d-1nal.html

Solubility

H2O

Smiles

N[C@@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N2CCC[C@H]2C(N[C@H](CC3=C4C=CC=CC4=CC=C3)C(O)=O)=O)=O)=O)CCCCN)=O)C/C=C\C1)=O)CO)=O)CC(C)C)=O)CCCNC(N)=N)=O

Molecular Formula

C49H73N13O11

Molecular Weight

1020.18

References & Citations

[1]Tran K, et, al. Size-Reduced Macrocyclic Analogues of [Pyr 1]-apelin-13 Showing Negative Gα 12 Bias Still Produce Prolonged Cardiac Effects. J Med Chem. 2022 Jan 13;65 (1) :531-551.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

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