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Technical Data
| Formula | C37H48N4O5 |
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| Molecular Weight | 628.8 | CAS No. | 192725-17-0 | |
| Solubility (25°C)* | In vitro | DMSO | 126 mg/mL (200.38 mM) | |
| Ethanol | 126 mg/mL (200.38 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. | ||
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| Targets |
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| In vitro | Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. [1] Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. [2] Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. [3] Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. [4] Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. [5] | ||
| In vivo | Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. [1] |
Protocol (from reference)
| Animal Study:[1] |
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References
Customer Product Validation
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Data from [Data independently produced by Antimicrob Agents Chemother, 2014, 58(8), 4875-84]
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Data from [Data independently produced by , , Biochim Biophys Acta, 2017, 1864(3):475-486]
Selleck's Lopinavir (ABT-378) has been cited by 46 publications
| Reactivated endogenous retroviruses promote protein aggregate spreading [ Nat Commun, 2023, 14(1):5034] | PubMed: 37596282 |
| Reactivated endogenous retroviruses promote protein aggregate spreading [ Nat Commun, 2023, 14(1):5034] | PubMed: 37596282 |
| Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062] | PubMed: 37047038 |
| Garbage in, garbage out: how reliable training data improved a virtual screening approach against SARS-CoV-2 MPro [ Front Pharmacol, 2023, 14:1193282] | PubMed: 37426813 |
| The Interleukin-11/IL-11 Receptor Promotes Glioblastoma Survival and Invasion under Glucose-Starved Conditions through Enhanced Glutaminolysis [ Int J Mol Sci, 2023, 24(4)3356] | PubMed: 36834778 |
| Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int. J. Mol. Sci, 2023, 10.3390/ijms24076062] | PubMed: None |
| Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
| The IDentif.AI-x pandemic readiness platform: Rapid prioritization of optimized COVID-19 combination therapy regimens [ NPJ Digit Med, 2022, 5(1):83] | PubMed: 35773329 |
| Cell-to-cell transmission of HIV-1 from provirus-activated cells to resting naïve and memory human primary CD4 T cells is highly efficient and requires CD4 and F-actin but not chemokine receptors [ J Med Virol, 2022, 10.1002/jmv.28005] | PubMed: 35840493 |
| Significant role of host sialylated glycans in the infection and spread of severe acute respiratory syndrome coronavirus 2 [ PLoS Pathog, 2022, 18(6):e1010590] | PubMed: 35700214 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.