Serlopitant
Serlopitant (VPD-737) is an orally active Neurokinin 1 receptor antagonist. Serlopitant inhibits pruritus signal transduction via NK receptors in spinal neurons and brain regions, and blocks the efferent function of substance P in the skin. Serlopitant can be used in research related to chronic pruritus, prurigo nodularis, and pruritus associated with psoriasis.
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- CAS. Nr.: 860642-69-9
- Formel: C29H28F7NO2
- Molecular Weight:555.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
|
NK1R |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.06 nM
Compound: 17
|
Displacement of [125I]substance P human recombinant NK1 receptor expressed in CHO cells in absence of human serum albumin
Displacement of [125I]substance P human recombinant NK1 receptor expressed in CHO cells in absence of human serum albumin
|
[PMID: 19354254] |
| CHO | IC50 |
0.06 nM
Compound: 2
|
Displacement of [125I]substance P from human NK1 receptor expressed in CHO cells
Displacement of [125I]substance P from human NK1 receptor expressed in CHO cells
|
[PMID: 23808489] |
| CHO | IC50 |
9.5 nM
Compound: 17
|
Displacement of [125I]substance P human recombinant NK1 receptor expressed in CHO cells in presence of human serum albumin
Displacement of [125I]substance P human recombinant NK1 receptor expressed in CHO cells in presence of human serum albumin
|
[PMID: 19354254] |
| CHO | IC50 |
9.5 nM
Compound: 2
|
Displacement of [125I]substance P from human NK1 receptor expressed in CHO cells in presence of human serum
Displacement of [125I]substance P from human NK1 receptor expressed in CHO cells in presence of human serum
|
[PMID: 23808489] |
Serlopitant induces a dose-dependent reduction in chronic pruritus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 860642-69-9
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Molecular Weight 555.53
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Formel C29H28F7NO2
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SMILES
O=C1C=C(N2C[C@@]3([H])CC[C@H](O[C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)[C@@H](C5=CC=C(F)C=C5)[C@]3([H])C2)CC1
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Synonyms
VPD-737; MK-0594
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)