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NH2-c[X-R-L-S-X]-K-G-P- (D-2Nal)

NH2-c[X-R-L-S-X]-K-G-P- (D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (Ki=5.7 nM) . NH2-c[X-R-L-S-X]-K-G-P- (D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life[1].

Product Specifications

CAS Number

2891469-81-9

UNSPSC

12352209

Target

Apelin Receptor (APJ)

Type

Peptides

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-2nal.html

Solubility

10 mM in DMSO

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=CC=C4C=CC=CC4=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

Peptides

Clinical Information

No Development Reported

Frequently Asked Questions

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