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Vebicorvir Sale

(Synonyms: ABI-H0731) 目录号 : GC63250

Vebicorvir (ABI-H0731) 是一代乙型肝炎病毒 (HBV) 核心蛋白的抑制剂。Vebicorvir (ABI-H0731) 共价抑制两个感染模型中cccDNA 的 EC50 值为 1.84-7.3 μM。

Vebicorvir Chemical Structure

Cas No.:2090064-66-5

规格 价格 库存 购买数量
5 mg
¥1,800.00
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10 mg
¥2,880.00
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25 mg
¥5,850.00
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50 mg
¥9,000.00
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产品描述

Vebicorvir (ABI-H0731) is a first-generation hepatitis B virus (HBV) core protein inhibitor. Vebicorvir (ABI-H0731) suppresses covalently closed circular DNA (cccDNA) formation in two de novo infection models with EC50s from 1.84 μM to 7.3 μM[1].

Vebicorvir (ABI-H0731) demonstrates inhibition of pgRNA, HBeAg, and HBsAg production, with EC50s of 2.68 μM, 4.95 μM, and 7.30 μM, respectively[1].Vebicorvir (ABI-H0731) is an inhibitor of pgRNA encapsidation and rcDNA synthesis[1].

After i.v. administration, the drug rapidly distributes and decayes in a biphasic manner in all species tested. Plasma clearance values of ABI-H0731 were 8.05, 10.1, 14.7, and 4.86 ml/min/kg, representing 9, 16, 47, and 11% of liver blood flow, in mouse, rat, dog, and monkey, respectively[1].

[1]. Qi Huang, et al. Preclinical Profile and Characterization of the Hepatitis B Virus Core Protein Inhibitor ABI-H0731. Antimicrob Agents Chemother. 2020 Oct 20;64(11):e01463-20.

Chemical Properties

Cas No. 2090064-66-5 SDF
别名 ABI-H0731
分子式 C19H12F3N3O4S2 分子量 467.44
溶解度 DMSO : 100 mg/mL (213.93 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mM 2.1393 mL 10.6966 mL 21.3931 mL
5 mM 0.4279 mL 2.1393 mL 4.2786 mL
10 mM 0.2139 mL 1.0697 mL 2.1393 mL
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Research Update

Safety and efficacy of Vebicorvir administered with entecavir in treatment-naïve patients with chronic hepatitis B virus infection

J Hepatol 2022 Nov;77(5):1265-1275.PMID:35697332DOI:10.1016/j.jhep.2022.05.027.

Background & aims: Nucleos(t)ide reverse transcriptase inhibitors do not completely suppress HBV DNA in chronic HBV infection (cHBV). Vebicorvir (VBR) is an investigational core inhibitor that interferes with multiple aspects of HBV replication. This phase II trial evaluated the safety and efficacy of VBR in combination with entecavir (ETV) in treatment-naïve patients with cHBV. Methods: HBeAg-positive, treatment-naïve patients without cirrhosis were randomised 1:1 in a double-blind manner to once-daily VBR 300 mg+ETV 0.5 mg or placebo (PBO)+ETV 0.5 mg for 24 weeks. The primary endpoint was change in mean log10 HBV DNA from Baseline to Week 12 and 24. Results: All patients in both treatment groups (PBO+ETV: 12/12; VBR+ETV: 13/13) completed the study. At Week 12, VBR+ETV led to a greater mean (SD) reduction from Baseline in log10 IU/ml HBV DNA (-4.45 [1.03]) vs. PBO+ETV (-3.30 [1.18]; p = 0.0077). At Week 24, VBR+ETV led to a greater reduction from Baseline in log10 IU/ml HBV DNA (-5.33 [1.59]) vs. PBO+ETV (-4.20 [0.98]; p = 0.0084). Greater mean reductions in pregenomic RNA were observed at Week 12 and 24 in patients receiving VBR+ETV vs. PBO+ETV (p <0.0001 and p <0.0001). Changes in viral antigens were similar in both groups. No drug interaction between VBR and ETV was observed. Two patients experienced HBV DNA rebound during treatment, with no resistance breakthrough detected. The safety of VBR+ETV was similar to PBO+ETV. All treatment-emergent adverse events and laboratory abnormalities were Grade 1/2. There were no deaths, serious adverse events, or evidence of drug-induced liver injury. Conclusions: In this 24-week study, VBR+ETV provided additive antiviral activity over PBO+ETV in treatment-naïve patients with cHBV, with a favourable safety and tolerability profile. Clinical trial number: NCT03577171 LAY SUMMARY: Hepatitis B is a long-lasting viral infection of the liver. Current treatments can suppress hepatitis B virus but do not offer the opportunity of cure, hence, new treatment approaches are required. Herein, we show that the combination of the novel core inhibitor Vebicorvir with an existing antiviral (entecavir) in treatment-naïve patients chronically infected with hepatitis B virus demonstrated greater antiviral activity than entecavir alone. Additionally, Vebicorvir was safe and well tolerated. Thus, further studies evaluating its potential role in the treatment of chronic hepatitis B are warranted.

Safety and efficacy of Vebicorvir in virologically suppressed patients with chronic hepatitis B virus infection

J Hepatol 2022 Sep;77(3):642-652.PMID:35460726DOI:10.1016/j.jhep.2022.04.005.

Background & aims: HBV nucleos(t)ide reverse transcriptase inhibitors (NrtIs) do not completely suppress HBV replication. Previous reports indicate persistent viremia during NrtI treatment despite HBV DNA being undetectable. HBV core inhibitors may enhance viral suppression when combined with NrtIs. This phase II trial (NCT03576066) evaluated the efficacy and safety of the investigational core inhibitor, Vebicorvir (VBR), in virologically- suppressed patients on NrtIs. Methods: Non-cirrhotic, NrtI-suppressed patients with chronic HBV were randomised to VBR 300 mg once daily or matching placebo (PBO) for 24 weeks. Treatment was stratified by hepatitis B e antigen (HBeAg) status. The primary endpoint was change from Baseline in serum HBeAg or hepatitis B surface antigen (HBsAg) after 24 weeks. Results: Of 73 patients enrolled, 47 were HBeAg positive and 26 were HBeAg negative. In HBeAg-positive and -negative patients, there were no differences in the change from Baseline at Week 24 for HBsAg or HBeAg. Using a novel, high-sensitivity assay to detect HBV DNA, a greater proportion of patients with detectable HBV DNA at Baseline achieved undetectable HBV DNA at Week 24 in the VBR+NrtI vs. PBO+NrtI group. In HBeAg-positive patients, a greater change from Baseline in HBV pregenomic (pg)RNA was observed at Week 24 with VBR+NrtI vs. PBO+NrtI. Treatment-emergent adverse events (TEAEs) in VBR+NrtI patients included upper respiratory tract infection, nausea, and pruritus. No serious adverse events, Grade 4 TEAEs, or deaths were reported. Conclusions: In this 24-week study, VBR+NrtI demonstrated a favourable safety and tolerability profile. While there were no significant changes in viral antigen levels, enhanced viral suppression was demonstrated by greater changes in DNA and pgRNA with the addition of VBR compared to NrtI alone. Clinical trials number: NCT03576066. Lay summary: Core inhibitors represent a novel approach for the treatment of chronic hepatitis B virus (HBV) infection, with mechanisms of action distinct from existing treatments. In this study, Vebicorvir added to existing therapy reduced HBV replication to a greater extent than existing treatment and was generally safe and well tolerated.