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.
For research use only. We do not sell to patients.
- CAS No.: 860642-69-9
- Formula: C29H28F7NO2
- Molecular Weight:555.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
NK1R |
Cellular Effect
|
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] |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 860642-69-9
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Molecular Weight 555.53
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Formula 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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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)
Keywords
- Serlopitant
- 860642-69-9
- VPD-737
- MK-0594
- VPD737
- VPD 737
- MK0594
- MK 0594
- MK-0594
- Neurokinin Receptor
- NK receptor
- Tachykinin receptor
- chronic pruritus
- chronic pruritus of unknown origin
- neurokinin 1 receptor
- brain region NK receptors
- prurigo nodularis
- substance P
- psoriatic pruritus
- spinal neuron
- skin
- Inhibitor
- inhibitor
- inhibit