LXR623 - CAS 875787-07-8
Catalog number:
B0084-460154
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H12ClF5N2
Molecular Weight:
422.78
COA:
Inquire
Targets:
LXR
Description:
WAY-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of LXR, which can reduces total serum cholesterol and LDL cholesterol and inhibits lesion growth in models of atherosclerosis. IC50 values= 24 and 179 nM (for LXRβ and LXRα, respectively)
Publictions citing BOC Sciences Products
  • >> More
Purity:
≥ 98.0%
Appearance:
White solid powder
Synonyms:
2-[(2-chloro-4-fluorophenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)indazole; 2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole; LXR 623; LXR-623; LXR623; WAY 252623; WAY-252623; WAY252623
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
MSDS:
Inquire
Application:
A novel and potent LXR (liverX receptor) β-agonist used as a potential candidate for the treatment of atopic dermatitis IC50 values= 24 and 179 nM (for LXRβ and LXRα, respectively)
Quality Standard:
In-house standard
Quantity:
Grams-Kilos
InChIKey:
KYWWJENKIMRJBI-UHFFFAOYSA-N
InChI:
1S/C21H12ClF5N2/c22-18-10-15(24)9-6-13(18)11-29-20(12-4-7-14(23)8-5-12)16-2-1-3-17(19(16)28-29)21(25,26)27/h1-10H,11H2
Canonical SMILES:
C1=CC2=C(N(N=C2C(=C1)C(F)(F)F)CC3=C(C=C(C=C3)F)Cl)C4=CC=C(C=C4)F
1.Biological Roles of Liver X Receptors in Immune Cells
Monica Pascual-Garcıa • Annabel F. Valledor. Arch. Immunol. Ther. Exp. (2012) 60:235–249
In addition to their role in sterol and glucose homeostasis, LXRs promote lipogenesis through the induction of sterol regulatory element-binding protein 1c (SREBP-1c) (Repa et al. 2000a) and carbohydrate response elementbinding protein (ChREBP) (Cha and Repa 2007). Both SREBP-1c and ChREBP are transcription factors that control the expression of molecules integral to fatty acid biosynthesis and esterification, and mice treated with panLXR agonists suffer a marked increase in plasma triglyceride levels (Schultz et al. 2000), which limit the potential therapeutic advantages of these agonists as anti-atherogenic or insulin-sensitizing drugs. Based on the fact that LXRa is more abundantly expressed than LXRb in the liver and accounts for most of the lipogenic effects of LXR agonists in this organ, alternative strategies try to identify compounds with higher selectivity for LXRb over LXRa to skip the hepatic lipogenic properties of general LXR agonists (Molteni et al. 2007; Ullrich et al. 2010). Also, two novel LXR agonists, WAY-252623 and N,N-dimethyl-3b-hydroxy-cholenamide, have been shown to reduce atherosclerotic lesion progression without inducing the expression of SREBP1c or activating hepatic lipogenesis, although the mechanisms involved in these selective actions have not been described (Kratzer et al. 2009; Quinet et al. 2009).
2.Liver X Receptors, Atherosclerosis and Inflammation
Daryn R. Michael & Tim G. Ashlin. Curr Atheroscler Rep (2012) 14:284–293
Currently, due to its progression towards phase I clinical trials, the most promising therapeutic target appears to be WAY-252623 (LXR-623), an indazole-based LXRβ modulator that has been shown to significantly reduce lesion progression in New Zealand white rabbits without affecting plasma cholesterol and triglyceride levels. Furthermore, WAY-252623 is also able to reduce plasma levels of total and LDL cholesterol and increase ABCA-1/G-1 expression in peripheral blood cells without having any marked effect on hepatic lipogenesis in cynomolgus monkeys. ABCA-1/G-1 expression levels have also been shown to be rapidly raised in the peripheral blood cells harvested from a representative human subject participating in an ongoing phase 1 SAD (Single Ascending Dose) clinical study of WAY-252623, suggesting that this agonist may be developed into a useful tool in the treatment of atherosclerosis.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related LXR Products


CAS 405911-17-3 GW3965 Hydrochloride

GW3965 Hydrochloride
(CAS: 405911-17-3)

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.

GSK-2033
(CAS: 1221277-90-2)

This active molecular is a cell permeable, potent LXR (liver-X-receptor) antagonist. pIC50 values is 7.0 for LXRα and 7.4 for LXRβ. GSK2033 enhances T-cell prol...

CAS 20380-11-4 27-Hydroxycholesterol

27-Hydroxycholesterol
(CAS: 20380-11-4)

27-Hydroxycholesterol, a desmosterol metabolite found in the brain , activates LXRα (EC50= 85 nM)and LXRβ (EC50= 71 nM) in vitro. 27-HC is also an estrogen rece...

SR9243
(CAS: 1613028-81-1)

SR9243 is a potent and selective LXR inverse agonist. SR9243 kills cancer cells by inhibiting lipid production and the Warburg effect.

CAS 405911-09-3 GW3965

GW3965
(CAS: 405911-09-3)

GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X rec...

CAS 30271-38-6 24-Hydroxycholesterol

24-Hydroxycholesterol
(CAS: 30271-38-6)

24-Hydroxycholesterol, also known as 24-OH-Chol, a natural sterol, is the main cholesterol elimination product of the brain. 24-Hydroxycholesterol is a positive...

CAS 875787-07-8 LXR623

LXR623
(CAS: 875787-07-8)

WAY-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of LXR, which can reduces total serum cholesterol and LDL cholesterol and...

Chemical Structure

CAS 875787-07-8 LXR623

Quick Inquiry

Verification code

Featured Items