GCA-186
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively.
For research use only. We do not sell to patients.
- CAS No.: 149950-61-8
- Formula: C19H26N2O3
- Molecular Weight:330.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CEM-SS | IC50 |
0.6 nM
Compound: 28
|
Tested for inhibitory concentration on HIV-I Lai wild type in CEM-SS cell line
Tested for inhibitory concentration on HIV-I Lai wild type in CEM-SS cell line
|
[PMID: 11052800] |
| CEM-SS | CC50 |
43 μM
Compound: 28
|
Tested for cytotoxic concentration on HIV-I Lai wild type in CEM-SS cell line
Tested for cytotoxic concentration on HIV-I Lai wild type in CEM-SS cell line
|
[PMID: 11052800] |
| HeLa | CC50 |
52.5 μM
Compound: GCA-186
|
Compound was tested for its cytotoxicity depending on the viability of mock-infected cells
Compound was tested for its cytotoxicity depending on the viability of mock-infected cells
|
[PMID: 10579814] |
| HeLa | EC50 |
0.001 μM
Compound: GCA-186
|
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like IIIB
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like IIIB
|
[PMID: 10579814] |
| HeLa | EC50 |
0.001 μM
Compound: GCA-186
|
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like NL4-3
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like NL4-3
|
[PMID: 10579814] |
| HeLa | EC50 |
0.04 μM
Compound: GCA-186
|
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like NL4-3K103N
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like NL4-3K103N
|
[PMID: 10579814] |
| HeLa | EC50 |
0.18 μM
Compound: GCA-186
|
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like IIIB-R(Y181C)
Compound was tested for its inhibition of HIV-1 induced focus formation in MAGI-CCR5 cells in strains like IIIB-R(Y181C)
|
[PMID: 10579814] |
| MT4 | IC50 |
0.001 μM
Compound: GCA-186
|
Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method
Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method
|
[PMID: 14643315] |
| MT4 | IC50 |
0.04 μM
Compound: GCA-186
|
Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method
Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method
|
[PMID: 14643315] |
| MT4 | IC50 |
0.18 μM
Compound: GCA-186
|
Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method
Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method
|
[PMID: 14643315] |
| MT4 | CC50 |
43 μM
Compound: 34
|
Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50%
Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50%
|
[PMID: 7636846] |
| MT4 | EC50 |
0.0006 μM
Compound: 34
|
Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 virus.
Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 virus.
|
[PMID: 7636846] |
| MT4 | EC50 |
0.6 nM
Compound: 34
|
Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 virus.
Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 virus.
|
[PMID: 7636846] |
Chemical Information
-
CAS No. 149950-61-8
-
Molecular Weight 330.42
-
Formula C19H26N2O3
-
SMILES
O=C1NC(C(C(C)C)=C(N1COCC)CC2=CC(C)=CC(C)=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. El-Brollosy NR, et al. Synthesis and antiviral evaluation of 6-(trifluoromethylbenzyl) and 6-(fluorobenzyl) analogues of HIV drugs emivirine and GCA-186. Arch Pharm (Weinheim). 2008;341(1):9-19. [Content Brief]
[2]. Hopkins AL, et al. Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants. J Med Chem. 1999;42(22):4500-4505. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)