2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. LXRβ ligand 1

LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC50 of 57 μM and a Ki of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators.

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

LXRβ ligand 1

LXRβ ligand 1 Chemical Structure

CAS No. : 171049-41-5

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10 mM * 1 mL in DMSO
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LXRβ ligand 1 Related Antibodies

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Description

LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC50 of 57 μM and a Ki of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators[1].

IC50 & Target

LXRβ

57 μM (EC50)

In Vitro

LXRβ ligand 1 (compound F3) activates purified human LXRβ-LBD to recruit coactivator peptides, with a potency of 23% relative to GW3965 (HY-10627)[1].
LXRβ ligand 1 binds to purified human LXRβ-LBD, and stabilizes the receptor in an active conformation via specific hydrogen bonding, hydrophobic interactions, and π-π stacking interactions[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LXRβ ligand 1 Related Antibodies
Molecular Weight

248.32

Formula

C14H20N2O2
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C(N1CC2=CC(N)=CC=C2CC1)OC(C)(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (201.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0271 mL 20.1353 mL 40.2706 mL
5 mM 0.8054 mL 4.0271 mL 8.0541 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.40%

SDS (394 KB)

COA (245 KB) HNMR (244 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0271 mL 20.1353 mL 40.2706 mL 100.6765 mL
5 mM 0.8054 mL 4.0271 mL 8.0541 mL 20.1353 mL
10 mM 0.4027 mL 2.0135 mL 4.0271 mL 10.0677 mL
15 mM 0.2685 mL 1.3424 mL 2.6847 mL 6.7118 mL
20 mM 0.2014 mL 1.0068 mL 2.0135 mL 5.0338 mL
25 mM 0.1611 mL 0.8054 mL 1.6108 mL 4.0271 mL
30 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3559 mL
40 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5169 mL
50 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0135 mL
60 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6779 mL
80 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2585 mL
100 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
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LXRβ ligand 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LXRβ ligand 1171049-41-5LXRβ ligand1LXRβ ligand-1LXRLiver X receptorLiver X receptor β ligand binding domainHis435co-activator peptidePhe329His-Trp activation switchhuman LXRβ-LBDInhibitorinhibitorinhibit

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