Abstract: Provided are an RNA inhibitor for inhibiting hepatitis B virus (HBV) gene expression and an application thereof. The RNA inhibitor is formed of a sense strand and an antisense strand by means of base pairing; the sense strand and the antisense strand are at least 85% complementary to each other, and —OH at 2? position of glycosyl of some or all of nucleotides is replaced by fluorine or methoxy, and phosphates between at least 3 consecutive nucleotides at the end are thioated. In the structure of the RNA inhibitor, 5?MVIP and 3?MVIP are also comprised, such that the RNA inhibitor has specific liver targeting. The RNA inhibitor can continuously inhibit the synthesis of an HBV surface antigen (HBsAg), can promote the production of HBV surface antibody (HBsAb), has an inhibitory effect on the most common types of HBV.

Abstract: The present invention relates to a novel compound and application thereof in the inhibition of HBV gene expression. The structure of the compound comprises an interfering nucleic acid for inhibiting HBV gene expression, transition points, and delivery chains of the interfering nucleic acid. By means of the delivery chains, two or three N-acetylgalactosamines can be introduced to an antisense strand 3? end of such siRNA, and two or one N-acetylgalactosamine can be correspondingly introduced to a sense strand 5? end, the total number of the introduced N-acetylgalactosamines being four. In vitro and in vivo pharmacological experiments prove that such a novel compound can continuously and efficiently inhibit HBV gene expression.

Abstract: The present invention relates to a novel compound and application thereof in the inhibition of HBV gene expression. The structure of the compound comprises an interfering nucleic acid for inhibiting HBV gene expression, transition points, and delivery chains of the interfering nucleic acid. By means of the delivery chains, two or three N-acetylgalactosamines can be introduced to an antisense strand 3? end of such siRNA, and two or one N-acetylgalactosamine can be correspondingly introduced to a sense strand 5? end, the total number of the introduced N-acetylgalactosamines being four. In vitro and in vivo pharmacological experiments prove that such a novel compound can continuously and efficiently inhibit HBV gene expression.

Abstract: The present invention relates to a novel compound and application thereof in the inhibition of HBV gene expression. The structure of the compound comprises an interfering nucleic acid for inhibiting HBV gene expression, transition points, and delivery chains of the interfering nucleic acid. By means of the delivery chains, two or three N-acetylgalactosamines can be introduced to an antisense strand 3? end of such siRNA, and two or one N-acetylgalactosamine can be correspondingly introduced to a sense strand 5? end, the total number of the introduced N-acetylgalactosamines being four. In vitro and in vivo pharmacological experiments prove that such a novel compound can continuously and efficiently inhibit HBV gene expression.