A potent NK1 receptor antagonist
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Rolapitant

Item No. 23906

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
CAS Number
552292-08-7
Molecular Formula
C25H26F6N2O2
Formula Weight
500.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH7.2) (1:2): 0.33 mg/mlDMSO: 16 mg/mlEthanol: 3 mg/ml
SMILES
C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)OC[C@@]2(C3=CC=CC=C3)CC[C@]4(CCC(N4)=O)CN2
InChi Code
InChI=1S/C25H26F6N2O2/c1-16(17-11-19(24(26,27)28)13-20(12-17)25(29,30)31)35-15-23(18-5-3-2-4-6-18)10-9-22(14-32-23)8-7-21(34)33-22/h2-6,11-13,16,32H,7-10,14-15H2,1H3,(H,33,34)/t16-,22-,23-/m1/s1
InChi Key
FIVSJYGQAIEMOC-ZGNKEGEESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $236

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    Product Description

    Rolapitant is a potent neurokinin-1 (NK1) receptor antagonist (Ki = 0.66 nM for the human receptor).1 It is greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels. Rolapitant inhibits GR-73632-induced calcium efflux in CHO cells expressing human NK1 in a concentration-dependent manner. In vivo, rolapitant inhibits GR-73632-induced foot-tapping in gerbils (ID90 = 0.3 mg/kg). It also prevents emesis in ferrets induced by apomorphine (Item No. 16094) and cisplatin (Item No. 13119) with ED50 values of 0.03 and 0.07 mg/kg, respectively. Formulations containing rolapitant have been used to prevent chemotherapy-induced nausea and vomiting.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Duffy, R.A., Morgan, C., Naylor, R., et al. Rolapitant (SCH 619734): A potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol. Biochem. Behav. 102(1), 95-100 (2012).