Product Name :
XL041
Description:
XL041 (BMS-852927) is an LXRβ-selective agonist.
CAS:
1256918-39-4
Molecular Weight:
609.51
Formula:
C29H28Cl2F2N2O4S
Chemical Name:
2-2-[2-(2,6-dichlorophenyl)propan-2-yl]-1-[3,3′-difluoro-4′-(hydroxymethyl)-5′-methanesulfonyl-[1,1′-biphenyl]-4-yl]-1H-imidazol-4-ylpropan-2-ol
Smiles :
CC(C)(O)C1=CN(C(=N1)C(C)(C)C1C(Cl)=CC=CC=1Cl)C1=CC=C(C=C1F)C1C=C(F)C(CO)=C(C=1)S(C)(=O)=O
InChiKey:
HNAJDMYOTDNOBK-UHFFFAOYSA-N
InChi :
InChI=1S/C29H28Cl2F2N2O4S/c1-28(2,26-19(30)7-6-8-20(26)31)27-34-25(29(3,4)37)14-35(27)23-10-9-16(11-22(23)33)17-12-21(32)18(15-36)24(13-17)40(5,38)39/h6-14,36-37H,15H2,1-5H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Cinacalcet Biological Activity
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
XL041 (BMS-852927) is an LXRβ-selective agonist.|Product information|CAS Number: 1256918-39-4|Molecular Weight: 609.51|Formula: C29H28Cl2F2N2O4S|Chemical Name: 2-2-[2-(2,6-dichlorophenyl)propan-2-yl]-1-[3,3′-difluoro-4′-(hydroxymethyl)-5′-methanesulfonyl-[1,1′-biphenyl]-4-yl]-1H-imidazol-4-ylpropan-2-ol|Smiles: CC(C)(O)C1=CN(C(=N1)C(C)(C)C1C(Cl)=CC=CC=1Cl)C1=CC=C(C=C1F)C1C=C(F)C(CO)=C(C=1)S(C)(=O)=O|InChiKey: HNAJDMYOTDNOBK-UHFFFAOYSA-N|InChi: InChI=1S/C29H28Cl2F2N2O4S/c1-28(2,26-19(30)7-6-8-20(26)31)27-34-25(29(3,4)37)14-35(27)23-10-9-16(11-22(23)33)17-12-21(32)18(15-36)24(13-17)40(5,38)39/h6-14,36-37H,15H2,1-5H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 100 mg/mL (164.Zandelisib PI3K 07 mM; Need ultrasonic).PMID:32841104 |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|XL041 (BMS-852927) is an LXRβ-selective agonist with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. XL041 is potent, with an EC50=9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively).|In Vivo:|XL041 (BMS-852927), has a very favorable profile at efficacious doses in cynomolgus monkeys and mice. XL041 pre-treatment of C57BL/6J mice for 7 days results in potent, dose-dependent stimulation of cholesterol efflux in this system, reaching a maximum in the 3 mg/kg/day dose group of 70% above vehicle in the initial efflux rate. Similar results are obtained in LDLR knockout (KO) mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO mice. Importantly, the dose response for inhibition of atherosclerosis (0.1-3 mg/kg/day) is similar to the dose response for macrophage reverse cholesterol transport (RCT) stimulation (0.03-3 mg/kg/day), a major underlying mechanism through which LXR agonists affect the disease.|Products are for research use only. Not for human use.|