1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. Rolapitant

Rolapitant (Synonyms: SCH619734)

Cat. No.: HY-14751 Purity: 98.43%
Handling Instructions

Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.

For research use only. We do not sell to patients.

Rolapitant Chemical Structure

Rolapitant Chemical Structure

CAS No. : 552292-08-7

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10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 150 In-stock
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25 mg USD 240 In-stock
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50 mg USD 400 In-stock
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100 mg USD 600 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.

IC50 & Target

Ki: 0.66 nM (neurokinin)[1]

In Vitro

Rolapitant has a high affinity for the human NK1 receptor with a Ki of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit[1].

In Vivo

Rolapitant reverses NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose (MED) of 0.1 mg/kg. Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, consistent with clinical data for other NK1 antagonists. Clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication[1].

Clinical Trial
Molecular Weight

500.48

Formula

C₂₅H₂₆F₆N₂O₂

CAS No.

552292-08-7

SMILES

C[[email protected]@](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)([H])OC[[email protected]@]2(C3=CC=CC=C3)CC[[email protected]@](CCC4=O)(N4)CN2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (59.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9981 mL 9.9904 mL 19.9808 mL
5 mM 0.3996 mL 1.9981 mL 3.9962 mL
10 mM 0.1998 mL 0.9990 mL 1.9981 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Rolapitant is made at a stock concentration of 1 mM in 100% DMSO. For most receptor binding studies, the stock solution is diluted with the final concentrations ranged from 0.1 to 3 μM. Radioligand concentrations for competition binding studies ranged from 0.5 to 1 nM. For species comparison studies, 150 pM [125I]-BHSP is incubated with varying concentrations of protein (10-50 μg) prepared from gerbil, rabbit and monkey striata, and from cells expressing cloned rat, mouse and guinea pig NK receptors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

RolapitantSCH619734SCH 619734SCH-619734Neurokinin ReceptorNK receptorInhibitorinhibitorinhibit

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Rolapitant
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