| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Lopinavir (formerly known as ABT-378; trade names Kaletra; Aluvia), an FDA approved antiretroviral drug in 2000 for HIV treatment, is a highly potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. Lopinavir is an analog of ritonavir intended to have less interaction with HIV protease's Val82. With a 50% effective concentration and an EC50 value less than 0.06 μM, it continues to have high potency in inhibiting the Val82 mutant HIV that was chosen using ritonavir. While human serum significantly reduces the antiviral activity of ritonavir, lopinavir is less affected by human serum proteins and remains 10-fold more potent than ritonavir when human serum is present. Marketed under the trade names Kaletra and Aluvia, lopinavir is used in a fixed-dose combination with another protease inhibitor, Ritonavir, to treat HIV infections.
| Targets |
HIV protease (Ki = 1.3 pM)
|
||
|---|---|---|---|
| ln Vitro |
Lopinavir has a Ki of 4.9 pM, 3.7 pM, and 3.6 pM for each of the mutant HIV proteases (V82A, V82F, and V82T). 93% of wild-type HIV protease activity is inhibited by lopinavir at 0.5 nM. With an EC50 of 17 nM and 102 nM, respectively, lopinavir inhibits HIV protease activity in MT4 cells both in the presence and absence of 50% HS. The conversion of lopinavir to multiple metabolites, namely M-3 and M-4, occurs in a manner that is dependent on NADPH in liver microsomes. Lopinavir, with an IC50 of 1.7 mM, is a strong inhibitor of Rh123 efflux in Caco-2 monolayers. In LS 180V cells, exposure tolopinavir for 72 hours lowers the amount of intracellular Rh123. In LS 180V cells, lopinavir increases the levels of messenger RNA and P-glycoprotein immunoreactive protein. [3] With an IC50 of 9.4 nM, lopinavir inhibits subtype C clone C6. [4] In human liver microsomes, lopinavir inhibits CYP3A with an IC50 of 7.3 mM, but it barely inhibits human CYP1A2, 2B6, 2C9, 2C19, and 2D6. [5]
|
||
| ln Vivo |
Lopinavir (10 mg/kg, orally) has an oral bioavailability of 25% and a Cmax of 0.8 μg/mL in rats.[1]
|
||
| Enzyme Assay |
Lopinavir is a potent inhibitor of HIV protease, with a Ki of 1.3 pM. Phospholipid HIV IC50 of 1.7 mM indicates thatlopinavir is a strong inhibitor of Rh123 efflux in Caco-2 monolayers.
|
||
| Cell Assay |
In LS 180V cells, lopinavir exposure (72 hours) lowers the amount of intracellular Rh123. In LS 180V cells, lopinavir increases the levels of messenger RNA and P-glycoprotein immunoreactive protein. With an IC50 of 9.4 nM, lopinavir inhibits subtype C clone C6. In human liver microsomes, lopinavir inhibits CYP3A with an IC50 of 7.3 mM, but it barely inhibits human CYP1A2, 2B6, 2C9, 2C19, and 2D6.
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C37H48N4O5
|
|---|---|
| Molecular Weight |
628.8
|
| Exact Mass |
628.36
|
| Elemental Analysis |
C, 70.67; H, 7.69; N, 8.91; O, 12.72
|
| CAS # |
192725-17-0
|
| Related CAS # |
(rel)-Lopinavir-d8;1322625-54-6;Lopinavir-d8;1224729-35-4
|
| Appearance |
Solid powder
|
| SMILES |
CC1=C(C(=CC=C1)C)OCC(=O)N[C@@H](CC2=CC=CC=C2)[C@H](C[C@H](CC3=CC=CC=C3)NC(=O)[C@H](C(C)C)N4CCCNC4=O)O
|
| InChi Key |
KJHKTHWMRKYKJE-SUGCFTRWSA-N
|
| InChi Code |
InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1
|
| Chemical Name |
(2S)-N-[(2S,4S,5S)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
|
| Synonyms |
Lopinavir; ABT-378; Aluviran; Koletra; ABT 378; A-157378.0; A157378.0; A 157378.0; ABT-378; ABT378; ABT 378
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 25 mg/mL (39.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 250.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL Solubility in Formulation 4: 20 mg/mL (31.81 mM) in Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5903 mL | 7.9517 mL | 15.9033 mL | |
| 5 mM | 0.3181 mL | 1.5903 mL | 3.1807 mL | |
| 10 mM | 0.1590 mL | 0.7952 mL | 1.5903 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
