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[CAS NO. 1155419-89-8] BI224436
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18595 |
| Brand: | MCE |
| CAS: | 1155419-89-8 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 442.51 |
| Molecular Formula | C27H26N2O4 |
| SMILES | CC1=C([C@@H](C(O)=O)OC(C)(C)C)[C@@]([C@@]2=CC=C3C4=C2N=CC=C4CCO3)=C5C(C=CC=C5)=N1 |
5 Publications Citing Use of MCE
Summary
IC50 & Target
EC50: 15 nM (HIV-1) [1]
In Vitro
BI 224436 has cellular cytotoxicity of more than 90 μM. BI 224436 has a low, 2.1-fold decrease in antiviral potency in the presence of 50% human serum. BI 224436 retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q. BI 224436 displays an additive effect in combination with most approved antiretrovirals, including INSTIs. BI 224436 has drug-like in vitro absorption, distribution, metabolism, and excretion (ADME) properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BI 224436 exhibits excellent pharmacokinetic profiles in rat (clearance as a percentage of hepatic flow [CL], 0.7%; bioavailability [F], 54%), monkey (CL, 23%; F, 82%), and dog (CL, 8%; F, 81%) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02183662 | Boehringer Ingelheim |
Healthy
|
November 2009 | Phase 1 |
| NCT01276990 | Boehringer Ingelheim |
HIV Infections|Healthy
|
January 2011 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years |
* The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 112.99 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2598 mL | 11.2992 mL | 22.5984 mL |
| 5 mM | 0.4520 mL | 2.2598 mL | 4.5197 mL |
| 10 mM | 0.2260 mL | 1.1299 mL | 2.2598 mL |
Synonyms
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