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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 860642-69-9
- Formule: C29H28F7NO2
- Masse moléculaire:555.53
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
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 No. 860642-69-9
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Masse moléculaire 555.53
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)