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BCP01757's Information

CAS NO. 871038-72-1 structure
Product Name Raltegravir potassium
Synonyms MK-0518;Raltegravir Potassium Salt;Raltegravir
Formula C20H20FKN6O5
Molecular Weight 444.41
Spec / Purity 98%
Supply Capacity can supply large quantity in kgs scale
Product Description Raltegravir Potassium Salt is a potent human immunodeficiency virus (HIV) integrase inhibitor
Details PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a ~twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31?0 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication. In acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range.

Price Info Please inquire us for bulk quantity, thanks.
size Price Stock
1 KG
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GET QUOTE
10 MG
US$115.60
Maintained in stock
500 MG
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Maintained in stock

Quality Control
Batch No. File Type File Name

PI3K/Akt/mTOR
Cell Cycle/Checkpoint
Angiogenesis/Tyrosine Kinase
Apoptosis Pathway
PARP/BET
Aurora/Ksp Pathway
MAPK Pathway
Hormone Pathay
Integrase/CCR5
Proteases/HSP90/HSP70 Pathway
Wnt/Hedgehog/Notch Pathway
Jak/Stat Pathway
Ca/cAMP/Lipid Signaling Pathway
Neuro Signaling Pathway
TGF-beta/Smad Signaling Pathway
GPCR Pathway
Ion channel Pathway
Cytochrome P450 Pathway
Others Pathway
Intermediate