Raltegravir (potassium salt)|cas 871038-72-1|DC Chemicals

Cas No.:	871038-72-1
Chemical Name:	Raltegravir potassium
Synonyms:	MK0518; MK 0518; MK-0518; HSDB-8124; HSDB 8124; HSDB8124; Raltegravir; brand name: Isentress
SMILES:	O=C(C(N=C(C(NC(C1=NN=C(C)O1)=O)(C)C)N2C)=C([O-])C2=O)NCC3=CC=C(F)C=C3.[K+]
Formula:	C₂₀H₂₀FKN₆O₅
M.Wt:	482.51
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Raltegravir potassium salt(MK0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection. Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. 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 induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy. 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.

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