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Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC. Pirmitegravir inhibits PBMC.Pirmitegravir has significant antiviral activity and may be useful in the study of HIV virus infection.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $136 | In Stock | |
5 mg | $338 | In Stock | |
10 mg | $546 | In Stock | |
25 mg | $1,090 | In Stock | |
50 mg | $1,790 | In Stock | |
100 mg | $2,390 | In Stock |
Description | Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC. Pirmitegravir inhibits PBMC.Pirmitegravir has significant antiviral activity and may be useful in the study of HIV virus infection. |
Targets&IC50 | HIV-1:0.41 nM, CEMx174 cells:1.4 nM |
In vitro | In CEMx174 cells, Pirmitegravir demonstrates an IC50 of 1.4 nM, inhibiting dual tropic HIV-189.6[1]. Pirmitegravir is a highly potent ALLINI, inhibiting both wild-type and Ral-resistant HIV-1 strains, with IC50 values ranging from picomolar to single-digit nanomolar[1].With an IC50 of 0.41 nM against HIV-1NL4-3, Pirmitegravir exhibits no observable cytotoxicity in human PBMCs at 10 μM (TC50 >10μM)[1]. |
In vivo | For once-daily administration, Pirmitegravir exhibits appropriate PK profiles[1]. The lack of micronucleus-inducing and bone marrow cell proliferation inhibitory potentials in rats (500, 1000, and 2000 mg/kg/day) supports the conclusion that Pirmitegravir is not genotoxic[1].An assessment of the Pharmacokinetics (PK) profile of Pirmitegravir in rat and dog has been conducted[1]. |
Alias | STP0404 |
Molecular Weight | 495.01 |
Formula | C27H31ClN4O3 |
Cas No. | 2245231-10-9 |
Smiles | [C@@H](OC(C)(C)C)(C(O)=O)C=1C(=C2C(N(CC=3C=NN(C)C3)C(C)=C2C)=NC1C)C4=CC=C(Cl)C=C4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (111.11 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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