Basic information Safety Supplier Related

GS9620

Basic information Safety Supplier Related

GS9620 Basic information

Product Name:
GS9620
Synonyms:
  • CS-925
  • GS 9620; GS9620
  • Vesatolimod
  • GS9620, >=98%
  • 4-amino-2-butoxy-8-[[3-(pyrrolidin-1-ylmethyl)phenyl]methyl]-5,7-dihydropteridin-6-one
  • 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one
  • 4-Amino-2-butoxy-8-[3-(1-pyrrolidinylmethyl)benzyl]-7,8-dihydro-6(5H)-pteridinone
  • GS 9620
CAS:
1228585-88-3
MF:
C22H30N6O2
MW:
410.51
Product Categories:
  • API
Mol File:
1228585-88-3.mol
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GS9620 Chemical Properties

Density 
1.247±0.06 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (10 mg/ml)
form 
solid
pka
10.34±0.20(Predicted)
color 
Off-white
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChIKey
VFOKSTCIRGDTBR-UHFFFAOYSA-N
SMILES
N1=C2C(NC(=O)CN2CC2=CC=CC(CN3CCCC3)=C2)=C(N)N=C1OCCCC
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GS9620 Usage And Synthesis

Description

GS-9620 is a potent and selective oral Toll-like receptor 7 (TLR7) agonist that directly activates plasmacytoid dendritic cells (pDCs). GS-9620 suppressed hepatitis B virus (HBV) in animal models of chronic infection and transiently activated HIV expressionex vivoin latently-infected peripheral blood mononuclear cells (PBMCs) from virally suppressed patients. Currently, GS-9620 is under clinical evaluation for treating chronic HBV infection and for reducing latent reservoirs in virally-suppressed HIV-infected patients.

Uses

Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

in vivo

Single oral doses of Vesatolimod (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 IFN-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), Vesatolimod (GS-9620) Cmax is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum IFN 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. Vesatolimod (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[2].

target

TLR-7

References

Lopatin, U, et al. "Safety, pharmacokinetics and pharmacodynamics of GS-9620, an oral Toll-like receptor 7 agonist." Antiviral Therapy18.3(2013):409-18.
Gane, E. J., et al. "The oral toll-like receptor-7 agonist GS-9620 in patients with chronic hepatitis B virus infection." Journal of Hepatology63.2(2015):320.
Lanford, Robert E., et al. "GS-9620, an Oral Agonist of Toll-Like Receptor-7, Induces Prolonged Suppression of Hepatitis B Virus in Chronically Infected Chimpanzees." Gastroenterology 144.7(2013):1508.

GS9620Supplier

Changzhou Chenhong Biotechnology Co., Ltd. Gold
Tel
+86-0519-85788828 +86-13775037613
Email
sales@chemrenpharm.com
Chengdu Celes Technology Co., Ltd Gold
Tel
19982073091
Email
2538834896@qq.com
Deyang Sino Biotech. Co., LTD Gold
Tel
+86-19182167371 +86-19182167371;
Email
service@synlord.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
shanghai Rainbow MediTech.Co.Ltd.
Tel
021-64968085,64968086-5815,5812; 13472757003
Email
xiaoxia.zeng@rainbowpharma.cn
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GS9620(1228585-88-3)Related Product Information