Vicriviroc
Vicriviroc (SCH 417690) is an orally active CCR5 antagonist with the IC50 of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC50 values of 0.91 nM and 16 nM,,respectively. Vicriviroc can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer.
For research use only. We do not sell to patients.
- CAS No.: 306296-47-9
- Formula: C28H38F3N5O2
- Molecular Weight:533.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
>5 μM
Compound: SCH-D
|
Cytotoxicity against human MT4 cells by MTT assay
Cytotoxicity against human MT4 cells by MTT assay
|
[PMID: 26094944] |
| MT4 | CC50 |
>5 μM
Compound: SCH-D
|
Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine
Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine
|
[PMID: 26094944] |
| MT4 | CC50 |
>5 μM
Compound: SCH-D; Sch-417690
|
Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
|
[PMID: 32305183] |
| MT4 | CC50 |
>5 μM
Compound: SCH-D; Sch-417690
|
Cytotoxicity against in human MT-4 after 5 days by MTT assay
Cytotoxicity against in human MT-4 after 5 days by MTT assay
|
[PMID: 33316719] |
| MT4 | EC50 |
>5 μM
Compound: SCH-D
|
Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay
Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay
|
[PMID: 26094944] |
| MT4 | EC50 |
>5 μM
Compound: SCH-D
|
Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine
Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine
|
[PMID: 26094944] |
| PBMC | IC50 |
0.23 nM
Compound: Sch-D
|
Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
|
[PMID: 24900235] |
| PBMC | IC50 |
0.56 nM
Compound: Sch-D
|
Antiviral activity against HIV-1 ADA infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
Antiviral activity against HIV-1 ADA infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
|
[PMID: 24900235] |
| PBMC | IC50 |
1.2 nM
Compound: Sch-D
|
Antagonist activity at CCR5 in IL-10 stimulated human PBMC cells assessed as MIP-1beta induced chemotaxis
Antagonist activity at CCR5 in IL-10 stimulated human PBMC cells assessed as MIP-1beta induced chemotaxis
|
[PMID: 24900235] |
Chemical Information
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CAS No. 306296-47-9
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Molecular Weight 533.63
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Formula C28H38F3N5O2
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SMILES
COC[C@@H](C1=CC=C(C=C1)C(F)(F)F)N2[C@H](CN(C3(CCN(CC3)C(C4=C(C)N=CN=C4C)=O)C)CC2)C
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Synonyms
SCH 417690; SCH-D; MK-7690 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca2+]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca2+ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
[1]. Strizki JM, et al. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2005;49(12):4911-4919. [Content Brief]
[2]. Bessudo A, et al. Safety and Efficacy of Vicriviroc (MK-7690) in Combination With Pembrolizumab in Patients With Advanced or Metastatic Microsatellite Stable Colorectal Cancer. Clin Colorectal Cancer. 2024;23(3):285-294. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)