Vesatolimod
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MedKoo CAT#: 206456

CAS#: 1228585-88-3

Description: Vesatolimod, also known as GS-9620, is a potent and oral agonist of Toll-like receptor-7 developed for finite treatment of chronic hepatitis B viral (HBV) infection, with the goal of inducing a liver-targeted antiviral effect without inducing the adverse effects associated with current systemic interferon-α (IFN-α) therapies. GS-9620 demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses. GS-9620 can induce a sustained antiviral response in the woodchuck model of CHB.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2950
Size
Price

25mg
USD 250
200mg
USD 1050
2g
USD 4250
Size
Price

50mg
USD 450
500mg
USD 1950
5g
Ask price

Vesatolimod, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206456
Name: Vesatolimod
CAS#: 1228585-88-3
Chemical Formula: C22H30N6O2
Exact Mass: 410.24302
Molecular Weight: 410.52
Elemental Analysis: C, 64.37; H, 7.37; N, 20.47; O, 7.79


Synonym: GS-9620; GS 9620; GS9620; Vesatolimod

IUPAC/Chemical Name: 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one

InChi Key: VFOKSTCIRGDTBR-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C1NC2=C(N)N=C(OCCCC)N=C2N(CC3=CC=CC(CN4CCCC4)=C3)C1


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Cohen J. Drug flushes out hidden AIDS virus. Science. 2015 Mar 6;347(6226):1056. doi: 10.1126/science.347.6226.1056-a. PubMed PMID: 25745141.

2: Gane EJ, Lim YS, Gordon SC, Visvanathan K, Sicard E, Fedorak RN, Roberts S, Massetto B, Ye Z, Pflanz S, Garrison KL, Gaggar A, Mani Subramanian G, McHutchison JG, Kottilil S, Freilich B, Coffin CS, Cheng W, Kim YJ. The oral toll-like receptor-7 agonist GS-9620 in patients with chronic hepatitis B virus infection. J Hepatol. 2015 Aug;63(2):320-8. doi: 10.1016/j.jhep.2015.02.037. Epub 2015 Feb 27. PubMed PMID: 25733157.

3: Menne S, Tumas DB, Liu KH, Thampi L, AlDeghaither D, Baldwin BH, Bellezza CA, Cote PJ, Zheng J, Halcomb R, Fosdick A, Fletcher SP, Daffis S, Li L, Yue P, Wolfgang GH, Tennant BC. Sustained efficacy and seroconversion with the Toll-like receptor 7 agonist GS-9620 in the Woodchuck model of chronic hepatitis B. J Hepatol. 2015 Jun;62(6):1237-45. doi: 10.1016/j.jhep.2014.12.026. Epub 2015 Jan 2. PubMed PMID: 25559326; PubMed Central PMCID: PMC4439359.

4: Lawitz E, Gruener D, Marbury T, Hill J, Webster L, Hassman D, Nguyen AH, Pflanz S, Mogalian E, Gaggar A, Massetto B, Subramanian GM, McHutchison JG, Jacobson IM, Freilich B, Rodriguez-Torres M. Safety, pharmacokinetics and pharmacodynamics of the oral Toll-like receptor 7 agonist GS-9620 in treatment-naive patients with chronic hepatitis C. Antivir Ther. 2014 Aug 8. doi: 10.3851/IMP2845. [Epub ahead of print] PubMed PMID: 25105516.

5: Fosdick A, Zheng J, Pflanz S, Frey CR, Hesselgesser J, Halcomb RL, Wolfgang G, Tumas DB. Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses. J Pharmacol Exp Ther. 2014 Jan;348(1):96-105. doi: 10.1124/jpet.113.207878. Epub 2013 Oct 16. PubMed PMID: 24133297.

6: Roethle PA, McFadden RM, Yang H, Hrvatin P, Hui H, Graupe M, Gallagher B, Chao J, Hesselgesser J, Duatschek P, Zheng J, Lu B, Tumas DB, Perry J, Halcomb RL. Identification and optimization of pteridinone Toll-like receptor 7 (TLR7) agonists for the oral treatment of viral hepatitis. J Med Chem. 2013 Sep 26;56(18):7324-33. doi: 10.1021/jm400815m. Epub 2013 Sep 9. PubMed PMID: 23961878.

7: Zoulim F, Luangsay S, Durantel D. Targeting innate immunity: a new step in the development of combination therapy for chronic hepatitis B. Gastroenterology. 2013 Jun;144(7):1342-4. doi: 10.1053/j.gastro.2013.04.028. PubMed PMID: 23710602.

8: Rosania K. Relying on chimpanzees for hepatitis research. Lab Anim (NY). 2013 Jun;42(6):188. doi: 10.1038/laban.317. PubMed PMID: 23689445.

9: Lopatin U, Wolfgang G, Tumas D, Frey CR, Ohmstede C, Hesselgesser J, Kearney B, Moorehead L, Subramanian GM, McHutchison JG. Safety, pharmacokinetics and pharmacodynamics of GS-9620, an oral Toll-like receptor 7 agonist. Antivir Ther. 2013;18(3):409-18. doi: 10.3851/IMP2548. Epub 2013 Feb 15. PubMed PMID: 23416308.

10: Lanford RE, Guerra B, Chavez D, Giavedoni L, Hodara VL, Brasky KM, Fosdick A, Frey CR, Zheng J, Wolfgang G, Halcomb RL, Tumas DB. GS-9620, an oral agonist of Toll-like receptor-7, induces prolonged suppression of hepatitis B virus in chronically infected chimpanzees. Gastroenterology. 2013 Jun;144(7):1508-17, 1517.e1-10. doi: 10.1053/j.gastro.2013.02.003. Epub 2013 Feb 13. PubMed PMID: 23415804; PubMed Central PMCID: PMC3691056.