| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
By using a gel assay, HIV-1 integrase inhibitor 8 has IC50 values of 275 µM and 200 µM for 3′-processing (TC) and strand-transfer (ST) activities in the presence of Mn2+ as the cationic cofactor, respectively. With an IC50 value of 200 µM, it inhibits the strand-transfer (ST) activity[1]. Gel electrophoresis is used to track the DNA relaxing activity of MCV topoisomerase, whilst a microtiter assay was used to track the DNA cleavage and religation activities. HIV-1 integrase inhibitor 8 has IC50 values of 500 µM and 200 µM, respectively, for inhibiting MCV topoisomerase and DNA religation. This finding shows that compound 8 is not effective against topoisomerase in any of the two assays[1]. In HeLa cells, HIV-1 integrase inhibitor 8 causes cytotoxicity and has an LD50 (dosage at which cell death reduces the signal by50%) of 20 μM[1].
|
|---|---|
| References |
| Molecular Formula |
C21H24O2
|
|---|---|
| Molecular Weight |
308.41
|
| Exact Mass |
308.178
|
| CAS # |
1568-80-5
|
| PubChem CID |
74071
|
| Appearance |
White to off-white solid powder
|
| Density |
1.21±0.1 g/cm3(Predicted)
|
| Boiling Point |
478.5℃ at 760 mmHg
|
| Melting Point |
213-214 °C
|
| Flash Point |
220.4℃
|
| Vapour Pressure |
8.84E-10mmHg at 25°C
|
| LogP |
4.746
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
23
|
| Complexity |
436
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SICLLPHPVFCNTJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H24O2/c1-19(2)11-21(17-9-13(22)5-7-15(17)19)12-20(3,4)16-8-6-14(23)10-18(16)21/h5-10,22-23H,11-12H2,1-4H3
|
| Chemical Name |
1,1,1',1'-tetramethyl-3,3'-spirobi[2H-indene]-5,5'-diol
|
| 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) |
DMSO: 125 mg/mL (405.30 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.74 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2424 mL | 16.2122 mL | 32.4244 mL | |
| 5 mM | 0.6485 mL | 3.2424 mL | 6.4849 mL | |
| 10 mM | 0.3242 mL | 1.6212 mL | 3.2424 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
