product name GS-9620
Description: GS-9620 (also known as NK-104 Calcium) is a potent and selective orally active small molecule agonist of Toll-like receptor 7. GS-9620 selectively induces IFN-α, cytokines and chemokines. The minimum effective concentrations for IFN-α induction were similar in pDCs and in PBMCs from HCV-positive donors. GS-9620 demonstrates an EC50 of 291 nM for human TLR7, which is 30-fold selectivity over TLR8 with EC50 of 9 μM.
References: Cardiol Rev. 2010 Sep-Oct;18(5):264-7; J Clin Invest. 2001 Jun;107(11):1423-32.
880.98
Formula
C50H46CaF2N2O8
CAS No.
147526-32-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 51 mg/mL (57.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
NK-104 Calcium
other peoduct :
| In Vitro |
In vitro activity: Pitavastatin significantly reduces both intracellular levels and synthesis of cholesterol esters. Pitavastatin is found to enhance LDL-receptor expression in vitro, as well as the amount of LDL binding to the LDL-receptor. Pitavastatin also exhibits more potent induction of LDL receptor mRNA expression compared with simvastatin and atorvastatin. Pitavastatin has many pleiotropic effects in vitro and in vivo, including deterring progression of atherosclerosis via inhibition of thromboxane synthesis, inhibition of migration/proliferation of vascular smooth muscle cells induced by angiotensin II, and stabilization of atherosclerotic plaque. Pitavastatin is able to activate PPARα and induce HDL apoA-I through inducing inhibition of the Rho-signaling pathway. Pitavastatin (1 μM) treatment for 48 h is able to enhances bone morphogenetic protein-2 BMP-2 (2.5-fold) and osteocalcin (10-fold) expression by inhibition of Rho-associated kinase in human osteoblasts. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Cardiol Rev. 2010 Sep-Oct;18(5):264-7; J Clin Invest. 2001 Jun;107(11):1423-32; Biochem Biophys Res Commun. 2001 Sep 21;287(2):337-42. |
