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BI 224436
CAS No. 1155419-89-8
BI 224436( BI224436 )
Catalog No. M10545 CAS No. 1155419-89-8
BI 224436 is a potent, specific, noncatalytic site integrase inhibitor (NCINI) of HIV-1 with EC50 of 11-27 nM against different HIV-1 laboratory strains.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 312 | Get Quote |
|
| 50MG | 1341 | Get Quote |
|
| 100MG | 1791 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameBI 224436
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NoteResearch use only, not for human use.
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Brief DescriptionBI 224436 is a potent, specific, noncatalytic site integrase inhibitor (NCINI) of HIV-1 with EC50 of 11-27 nM against different HIV-1 laboratory strains.
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DescriptionBI 224436 is a potent, specific, noncatalytic site integrase inhibitor (NCINI) of HIV-1 with EC50 of 11-27 nM against different HIV-1 laboratory strains, with minimal cellular cytotoxicity; exhibits a low, ～2.1-fold decrease in antiviral potency in the presence of 50% human serum andserum-shifted EC95 values ranging between 22 and 75 nM; also retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q; displays an additive effect in combination with most approved antiretrovirals, including INSTIs.HIV Infection Phase 1 Clinical.
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In VitroBI 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.
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In VivoBI 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%).
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SynonymsBI224436
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PathwayMicrobiology/Virology
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TargetHIV
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RecptorHIV
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Research AreaInfection
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IndicationHIV Infection
Chemical Information
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CAS Number1155419-89-8
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Formula Weight391.467
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Molecular FormulaC24H25NO4
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 50 mg/mL 112.99 mM
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SMILESO=C(O)[C@H](C1=C(C2=CC(CCCO3)=C3C=C2)C4=CC=CC=C4N=C1)OC(C)(C)C
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Chemical Name(2S)-[4-(3,4-Dihydro-2H-chromen-6-yl)-3-quinolinyl][(2-methyl-2-propanyl)oxy]acetic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Fader LD, et al. ACS Med Chem Lett. 2014 Jan 22;5(4):422-7.
2. Fenwick C, et al. Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44.
3. Demeulemeester J, et al. Expert Opin Ther Pat. 2014 Jun;24(6):609-32.
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