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Cat. No.: HY-12114

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Serlopitant

Name: Serlopitant
Brand: MedChemExpress
SKU: HY-12114
Availability: PreOrder

(Synonyms: VPD-737; MK-0594)

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.

Data Sheet (277 KB)

Serlopitant Chemical Structure

CAS No.: 860642-69-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Protocole (1)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

NK1R

Voir tous les produits spécifiques à Isoform Neurokinin Receptor :

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

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. Further protocols information, click here.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 860642-69-9
Masse moléculaire 555.53
Formule C₂₉H₂₈F₇NO₂
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
Synonyms

VPD-737; MK-0594
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocole

All Animals and Diseases

Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Yosipovitch G, et al. Serlopitant for the treatment of chronic pruritus: Results of a randomized, multicenter, placebo-controlled phase 2 clinical trial. J Am Acad Dermatol. 2018 May;78(5):882-891.e10. [Content Brief]

[2]. Ständer S, et al. The NK1 receptor antagonist serlopitant for treatment of chronic pruritus. Expert opinion on investigational drugs. 2019 Aug;28(8):659-666.

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Essai clinique
Chemical Information
Protocole
Pureté et documentation
Références

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Serlopitant

Voir tous les produits spécifiques à Isoform Neurokinin Receptor