[CAS NO. 2787501-83-9] AZD5462
PRODUCTS SPECIFICATIONS [2787501-83-9]
DESCRIPTION [2787501-83-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 544.65 |
| Molecular Formula | C30H41FN2O6 |
| SMILES | C[C@]1(C(O)=O)CC[C@@H](OC2=C(F)C=C(OC)C(C(N[C@@H]3[C@H](C4)CC[C@H]4[C@@H]3C(NCC5(CCC5)C)=O)=O)=C2)CC1 |
Summary
AZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, belongs to GPCR family 1c number with anti-fibrotic and anti-inflammatory properties [1] .
IC50 & Target
RXFP1 [1]
In Vitro
AZD5462 (example 1) shows stimulatory activity on cAMP or cGMP production with EC
50
s of 17 nM and 50 nM, respectively
[1]
.
AZD5462 binds human plasma protein with fraction unbound (free) rate of 4.3%, and shows the stability with Cl
int
values of 23 μL/min/mg (human licer microsomal), 4.8 μL/min/10
6
cells (human hepatocyte), and 11 μL/min/10
6
cells (rat hepatocyte)
[1]
.
AZD5462 enhances phosphorylation of ERK with an EC
50
value of 6.3 nM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04994106 | AstraZeneca |
Healthy Participants
|
July 27, 2021 | Phase 1 |
| NCT05512806 | AstraZeneca|Parexel |
Healthy Participants
|
August 24, 2022 | Phase 1 |
| NCT05395117 | AstraZeneca|Parexel |
Healthy Participants
|
June 30, 2022 | Phase 1 |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.