BMS-681
BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer.
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- CAS No.: 847998-92-9
- 화학식: C26H36F3N5O
- 분자량:491.59
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.8 μM
Compound: 13d
|
Inhibition of human ERG expressed in HEK293 cells assessed as reduction in peak tail current at holding potential of 80 mV to +20 mV by whole cell patch clamp assay
Inhibition of human ERG expressed in HEK293 cells assessed as reduction in peak tail current at holding potential of 80 mV to +20 mV by whole cell patch clamp assay
|
[PMID: 25893046] |
| HT-1080 | IC50 |
2.4 nM
Compound: 13d
|
Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs
Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs
|
[PMID: 25893046] |
Chemical Information
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CAS No. 847998-92-9
-
분자량 491.59
-
화학식 C26H36F3N5O
-
SMILES
O=C1N([C@@H]2[C@H](CCC)C[C@H](N(C(C)C)C)CC2)CC[C@@H]1NC3=C4C=C(C(F)(F)F)C=CC4=NC=N3
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Synonyms
BMS-687681
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)