CAS 1155419-89-8 BI 224436

BI 224436 - CAS 1155419-89-8

Catalog number: 1155419-89-8

Not Intended for Therapeutic Use. For research use only.

Molecular Formula:
Molecular Formula	C27H26N2O4
Molecular Weight:
Molecular Weight	442.51
COA:
COA	Inquire
Targets:
Targets	HIV
Description:
Description	BI 224436 is a novel HIV-1 non-catalytic-site integrase inhibitor; has antiviral EC50s of <15 nM against different HIV-1 laboratory strains and cellular cytotoxicity of >90 μM.

Publictions citing BOC Sciences Products

>> More

Purity:
Purity	>98%
MSDS:
MSDS	Inquire

1.Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.

Fader LD1, Malenfant E1, Parisien M1, Carson R1, Bilodeau F1, Landry S1, Pesant M1, Brochu C1, Morin S1, Chabot C1, Halmos T1, Bousquet Y1, Bailey MD1, Kawai SH1, Coulombe R1, LaPlante S1, Jakalian A1, Bhardwaj PK1, Wernic D1, Schroeder P1, Amad M1, Edwar ACS Med Chem Lett. 2014 Jan 22;5(4):422-7. doi: 10.1021/ml500002n. eCollection 2014.

An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization beginning with compound 1 established the importance of the C3 and C4 substituent to antiviral potency against viruses with different aa124/aa125 variants of IN. The importance of the C7 position on the serum shifted potency was established. Introduction of a quinoline substituent at the C4 position provided a balance of potency and metabolic stability. Combination of these findings ultimately led to the discovery of compound 26 (BI 224436), the first NCINI to advance into a phase Ia clinical trial.

2.Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.

Fenwick C1, Amad M2, Bailey MD2, Bethell R2, Bös M2, Bonneau P2, Cordingley M2, Coulombe R2, Duan J2, Edwards P2, Fader LD1, Faucher AM2, Garneau M2, Jakalian A2, Kawai S2, Lamorte L2, LaPlante S2, Luo L2, Mason S2, Poupart MA2, Rioux N2, Schroeder P2, Si Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44. doi: 10.1128/AAC.02719-13. Epub 2014 Mar 24.

BI 224436 is an HIV-1 integrase inhibitor with effective antiviral activity that acts through a mechanism that is distinct from that of integrase strand transfer inhibitors (INSTIs). This 3-quinolineacetic acid derivative series was identified using an enzymatic integrase long terminal repeat (LTR) DNA 3'-processing assay. A combination of medicinal chemistry, parallel synthesis, and structure-guided drug design led to the identification of BI 224436 as a candidate for preclinical profiling. It has antiviral 50% effective concentrations (EC50s) of <15 nM against different HIV-1 laboratory strains and cellular cytotoxicity of >90 μM. BI 224436 also has a low, ∼2.1-fold decrease in antiviral potency in the presence of 50% human serum and, by virtue of a steep dose-response curve slope, exhibits serum-shifted EC95 values ranging between 22 and 75 nM. Passage of virus in the presence of inhibitor selected for either A128T, A128N, or L102F primary resistance substitutions, all mapping to a conserved allosteric pocket on the catalytic core of integrase.

Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related HIV Products

Nevirapine
(CAS: 129618-40-2)

Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.

GS-7340 fumarate
(CAS: 379270-38-9)

Tenofovir alafenamide fumarate, also known as Tenofovir alafenamide hemifumarate; TAF, GS-7340, is a nucleotide reverse transcriptase inhibitor and a novel pro...

Darunavir Ethanolate
(CAS: 635728-49-3)

Darunavir Ethanolate is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.

Trovirdine
(CAS: 149488-17-5)

Trovirdine, a thiourea non-nucleoside reverse transcriptase inhibitor, was shown to inhibits HIV-1 RT when employing heteropolymeric primer/template (oligo-DNA/...

Brecanavir
(CAS: 313682-08-5)

Brecanavir is a tyrosyl-based arylsulfonamide, high-affinity, protease inhibitor (PI) for the treatment of human immunodeficiency virus type-1. This compound po...

Ebselen
(CAS: 60940-34-3)

Ebselen, also known as SPI-1005, is an organoselenium compound with potential anti-oxidant, anti-inflammatory and cytoprotective activity. Upon oral administra...

BI 224436
(CAS: 1155419-89-8)

BI 224436 is a novel HIV-1 non-catalytic-site integrase inhibitor; has antiviral EC50s of <15 nM against different HIV-1 laboratory strains and cellular cytotox...

Triciribine
(CAS: 35943-35-2)

Triciribine is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Akt-1, -2, and -3 are serine/th...

Tenofovir maleate
(CAS: 1236287-04-9)

Tenofovir hydrate reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. ...

CAS 226700-81-8 Fosamprenavir Calcium Salt

Fosamprenavir Calcium Salt
(CAS: 226700-81-8)

HIV protease inhibitor; water soluble prodrug of amprenavir.

Raltegravir
(CAS: 871038-72-1)

Raltegravir is a potent, selective, and orally bioavailable inhibitor of HIV integrase (IC50 = 15 nM). It is metabolized primarily by uridine diphosphate glucur...

BMS-707035
(CAS: 729607-74-3)

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM.

CAS 957890-42-5 HIV-1 integrase inhibitor 2

HIV-1 integrase inhibitor 2
(CAS: 957890-42-5)

HIV-1 integrase inhibitor 2 is useful for anti-HIV, which can target HIV-1 integrase and depress the activity in the treatment of HIV infection, AIDS, and other...

Tipranavir
(CAS: 174484-41-4)

Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against mult...

(±)-BI-D
(CAS: 1416258-16-6)

Approximately 2.4–2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160–200 ...

Elvitegravir
(CAS: 697761-98-1)

Elvitegravir (EVG, JTK-303/GS-9137) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

Lersivirine
(CAS: 473921-12-9)

Lersivirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for the treatment of HIV-1 infection. It prevents HIV ...

Efavirenz
(CAS: 154598-52-4)

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are highly specific and potent allosteric inhibitors of human immunodeficiency virus type 1 (HIV-1) rev...

Dolutegravir sodium
(CAS: 1051375-19-9)

Dolutegravir sodium salt is a HIV integrase inhibitor(IC50= 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G1...

BMS-626529
(CAS: 701213-36-7)

BMS-626529 is a member of the new drug class of HIV-1 attachment inhibitors currently in development. BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529...

Chemical Structure

Quick Inquiry

Name:

* Email:

* Service & Products of Interest:

* Quantity:

* Verification code:

Related HIV Products

Quick Inquiry

Featured Items

Drug Discovery

Chemistry

Life Science