RO5101576
RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guinea pigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guinea pigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated.
For research use only. We do not sell to patients.
- CAS No.: 1123155-95-2
- Formula: C36H38O8S
- Molecular Weight:630.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Endogenous Metabolite Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>3 μM
Compound: 33
|
Inhibition of human ERG expressed in CHO cells assessed as reduction of current amplitude
Inhibition of human ERG expressed in CHO cells assessed as reduction of current amplitude
|
[PMID: 20380377] |
| HEK293 | IC50 |
114 nM
Compound: 33
|
Antagonist activity at FLAG-tagged human BLT1 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge
Antagonist activity at FLAG-tagged human BLT1 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge
|
[PMID: 20380377] |
| HEK293 | IC50 |
164 nM
Compound: 33
|
Antagonist activity at FLAG-tagged human BLT2 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge
Antagonist activity at FLAG-tagged human BLT2 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge
|
[PMID: 20380377] |
| HL-60 | IC50 |
0.44 nM
Compound: 33
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Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins
Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins
|
[PMID: 20380377] |
| Neutrophil | IC50 |
0.1 nM
Compound: 33
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Inhibition of LTB4-stimulated human neutrophils migration after 30 mins by using CyQuant GR fluorescent dye
Inhibition of LTB4-stimulated human neutrophils migration after 30 mins by using CyQuant GR fluorescent dye
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[PMID: 20380377] |
Chemical Information
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CAS No. 1123155-95-2
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Molecular Weight 630.75
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Formula C36H38O8S
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SMILES
O=C(CCCOC1=CC=CC(CCCCCCOC2=CC(C3=CSC=C3)=CC(C4=CC=C5OCOC5=C4)=C2)=C1CCC(O)=O)O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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