[CAS NO. ] ERRαLigand-LinkerConjugates1

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PRODUCTS SPECIFICATIONS

Catalog

HY-130499

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	601.42
Molecular Formula	C24H20F9N3O5
SMILES	NCCNC(/C(C#N)=C/C1=CC(OC)=C(C=C1)OCC2=C(C(F)(F)F)C=C(C(F)(F)F)C=C2)=O.O=C(C(F)(F)F)O

For research use only. We do not sell to patients.

Summary

ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα) , and a PROTAC linker, which recruit E3 ligases MDM2 . ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs , such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader ^[1] .

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL ( 332.55 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6627 mL	8.3137 mL	16.6273 mL
5 mM	0.3325 mL	1.6627 mL	3.3255 mL
10 mM	0.1663 mL	0.8314 mL	1.6627 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 5 mg/mL (8.31 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 5 mg/mL (8.31 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Peng L, et al. Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation. ACS Med Chem Lett. 2019 Apr 12;10(5):767-772.