产品名称

英文名称：GS-9620

同义词

Vesatolimod、1228585-88-3、GS-9620、4-Amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one、GS9620、Vesatolimod [INN]、8-(3-(pyrrolidin-1-ylmethyl)benzyl)-4-amino-2-butoxy-7,8-dihydropteridin-6(5H)-one、CHEMBL2424780、O8M467C50G、MFCD25、4-氨基-2-丁氧基-7,8-二氢-8-[[3-(1-吡咯烷基甲基)苯基]甲基]-6(5H)-蝶啶酮

产品性质

CAS编号：1228585-88-3

分子式：C22H30N6O2

分子量：410.51

PubChem编号：46241268

别名：4-氨基-2-丁氧基-7,8-二氢-8-[[3-(1-吡咯烷基甲基)苯基]甲基]-6(5H)-蝶啶酮

英文别名：Vesatolimod|1228585-88-3|GS-9620|4-Amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one|GS9620|Vesatolimod [INN]|8-(3-(pyrrolidin-1-ylmethyl)benzyl)-4-amino-2-butoxy-7,8-dihydropteridin-6(5H)-one|CHEMBL2424780|O8M467C50G|MFCD25

规格或纯度：≥95%

英文名称：GS-9620

生化机理：Description IC50 Value N/A GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7(TLR-7) in chimpanzees with chronic HBV infection [1]. GS-9620 is a novel oral agonist of Toll-like receptor 7 (TLR7) in development for the treatment of chronic viral hepatitis. TLR7 is a highly conserved innate immune receptor expressed primarily on plasmacytoid dendritic cells and B lymphocytes [2]. in vitro N/A in vivo Short-term oral administration of GS-9620 provided long-term suppression of serum and liver HBV DNA. The mean maximum reduction of viral DNA was 2.2 logs, which occurred within 1 week of the end of GS-9620 administration; reductions of >1 log persisted for months. Serum levels of HBV surface antigen and HBV e antigen, and numbers of HBV antigen-positive hepatocytes, were reduced as hepatocyte apoptosis increased. GS-9620 administration induced production of interferon-α and other cytokines and chemokines, and activated interferon-stimulated genes, natural killer cells, and lymphocyte subsets [1]. Induction of chemokines/cytokines and IFN-stimulated genes were seen at GS-9620 doses ≥2 mg, well below doses that induced serum IFN-α or led to clinical adverse events [2]. Clinical trial A Study Evaluating GS-9620 in Treatment Naive Subjects With Chronic Hepatitis B. Phage1

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍SGC-CBP30是强效的CREBBP/EP300抑制剂，无细胞试验中IC50分别为21 nM 和 38 nM。对CBP的选择性分别是对BRD4(1)和BRD4(2)选择性的40倍和250倍。product descriptionGS-9620 is an effective and specific orally active agonist of Toll-like receptor 7.In vitro activityGS-9620 rapidly internalizes into cells and preferentially localizes to and signals from endo-lysosomal compartments. To test this hypothesis, the kinetics of cellular uptake of the compound in Daudi cells using tritiated GS-9620 (3H-GS-9620) is measured. The kinetics of 3H-GS-9620 accumulation is rapid, reaching concentration-dependent steady-state equilibrium in approximately thirty minutes. Measured intracellular concentration of 3H-GS-9620 is 5-fold higher than the extracellular concentration of 3H-GS-9620 used to treat cells. Increases in intracellular 3H-GS-9620 concentrations are roughly proportional with increasing concentrations of 3H-GS-9620In vivo activitySingle oral doses of GS-9620 at 0.3 and 1 mg/kg in uninfected chimpanzees demonstrates a dose- and exposure-related induction of serum IFN-α, select cytokines/chemokines, and interferon-stimulated genes (ISG) in the peripheral blood and liver. Following oral administration at 0.3 (n=3), and 1 mg/kg (n=3 and n=4), GS-9620 Cmax is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum interferon responses occur at 8 h post-dose. The mean peak levels of induced serum IFN-α are 66 and 479 pg/mL at doses of 0.3 and 1 mg/kg, respectively. GS-9620 treatment induces ISG transcripts including ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11) in peripheral blood mononuclear cells (PBMC) at 0.3 mg/kg and in both PBMC and the liver at 1 mg/kg.

ALogP：2.7

IUPAC Name：4-amino-2-butoxy-8-[[3-(pyrrolidin-1-ylmethyl)phenyl]methyl]-5,7-dihydropteridin-6-one

INCHI：InChI=1S/C22H30N6O2/c1-2-3-11-30-22-25-20(23)19-21(26-22)28(15-18(29)24-19)14-17-8-6-7-16(12-17)13-27-9-4-5-10-27/h6-8,12H,2-5,9-11,13-15H2,1H3,(H,24,29)(H2,23,25,26)

InChi Key：VFOKSTCIRGDTBR-UHFFFAOYSA-N

Canonical SMILES：CCCCOC1=NC(=C2C(=N1)N(CC(=O)N2)CC3=CC=CC(=C3)CN4CCCC4)N

Isomeric SMILES：CCCCOC1=NC(=C2C(=N1)N(CC(=O)N2)CC3=CC=CC(=C3)CN4CCCC4)N

PubChem CID：46241268

溶解性：DMSO mg/mL Water mg/mL Ethanol mg/mL

产品包装