871038-72-1
Raltegravir potassium
CAS: 871038-72-1
Molecular Formula: C20H20FN6O5.K
871038-72-1 - Names and Identifiers
| Name | Raltegravir potassium |
| Synonyms | CS-1293 MK 0518 CS-1950 MK 0518 MK0518 POTASSIUM SALT Raltegravir potassium MK 0518 POTASSIUM SALT MK 0518 potassium salt MK-0518 POTASSIUM SALT ISENTRESS POTASSIUM SALT Isentress potassium salt Raltegravir Potassium Salt N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide Potassium Salt N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide potassium salt |
| CAS | 871038-72-1 |
| EINECS | 682-461-3 |
| InChI | InChI=1/C20H21FN6O5.K/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11;/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30);/q;+1/p-1 |
871038-72-1 - Physico-chemical Properties
| Molecular Formula | C20H20FN6O5.K |
| Molar Mass | 482.511 |
| Melting Point | 155-157°C |
| Solubility | DMSO (Slightly, Heated), Methanol (Slightly, Heated), Water (Slightly) |
| Appearance | Solid |
| Color | White to Light Beige |
| Storage Condition | -20°C Freezer |
| In vitro study | PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC 50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC 50 of 200 nM, indicating a appr 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±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC 95 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 EC 90 in the low nanomolar range. |
| In vivo study | Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy. |
871038-72-1 - Risk and Safety
| HS Code | 2934990002 |
871038-72-1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.072 ml | 10.362 ml | 20.725 ml |
| 5 mM | 0.414 ml | 2.072 ml | 4.145 ml |
| 10 mM | 0.207 ml | 1.036 ml | 2.072 ml |
| 5 mM | 0.041 ml | 0.207 ml | 0.414 ml |
Last Update：2024-01-02 23:10:35
871038-72-1 - Reference Information
| biological activity | Raltegravir potasium is an orally active raltegravir Potassium salt. Raltegravr is a HIV-1 integrase inhibitor. |
| Target | Value |
Last Update：2024-04-09 20:48:19
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View History
871038-72-1
492431-11-5
(R)-3-CHLORO-1,2-PROPANEDIOL ACETONIDE
2-Fluoro-4-formylbenzoic acid
64034-01-1
LYPRESSIN
AMYL BENZOATE
UNII-EFY6W0M8TG
5-BroMo-3-(trifluoroMethyl)picolinonitrile
492431-11-5
(R)-3-CHLORO-1,2-PROPANEDIOL ACETONIDE
2-Fluoro-4-formylbenzoic acid
64034-01-1
LYPRESSIN
AMYL BENZOATE
UNII-EFY6W0M8TG
5-BroMo-3-(trifluoroMethyl)picolinonitrile