Apabetalone(RVX-08,RVX-000222)

Molecular Weight (MW)	370.4
Formula	C20H22N2O5
CAS No.	1044870-39-4
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 74 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)	0.5% CMC Na (1N HCl, PH 2.5-3.0): 8 mg/mL
Synonyms	RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone. Chemical Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one InChi Key: NETXMUIMUZJUTB-UHFFFAOYSA-N InChi Code: InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24) SMILES Code: O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3

Molecular Weight (MW)

370.4

Formula

C20H22N2O5

CAS No.

1044870-39-4

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 74 mg/mL (199.8 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In vivo)

0.5% CMC Na (1N HCl, PH 2.5-3.0): 8 mg/mL

Synonyms

RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone.

Chemical Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one

InChi Key: NETXMUIMUZJUTB-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24)

SMILES Code: O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3

In Vitro	In vitro activity: As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. Kinase Assay: Experiments are run on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. IC50 values are calculated in Prism 5 after normalization against corresponding DMSO controls. Assays are performed according to the manufacturer’s protocol with minor modifications. Cell Assay: HepG2 cells treated with RVX-208 (5 μM) for 4 h only modestly affected BET-dependent gene transcription. Moreover, RVX-208 increased apolipoprotein (apo)A-I and high-density lipoprotein cholesterol (HDL-C) levels in HepG2 cells.
In Vivo	RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways.
Animal model	Naive adult male AGMs
Formulation & Dosage	Dissolved in 1N HCl and carboxymethyl cellulose; 60mg/kg; i.v. injection or p.o.
References	Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9; Curr Opin Investig Drugs. 2010 Mar;11(3):357-64; J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9.

In Vitro

In vitro activity: As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro.

Kinase Assay: Experiments are run on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. IC50 values are calculated in Prism 5 after normalization against corresponding DMSO controls. Assays are performed according to the manufacturer’s protocol with minor modifications.

Cell Assay: HepG2 cells treated with RVX-208 (5 μM) for 4 h only modestly affected BET-dependent gene transcription. Moreover, RVX-208 increased apolipoprotein (apo)A-I and high-density lipoprotein cholesterol (HDL-C) levels in HepG2 cells.

In Vivo

RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways.

Animal model

Naive adult male AGMs

Formulation & Dosage

Dissolved in 1N HCl and carboxymethyl cellulose; 60mg/kg; i.v. injection or p.o.

References

Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9; Curr Opin Investig Drugs. 2010 Mar;11(3):357-64; J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9.

CAS NO:	1044870-39-4
规格:	≥98%

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议