An antiemetic and NK1 antagonist
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Pro-drug Form(s)
24034Fosaprepitant dimeglumine
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Aprepitant

Item No. 14867

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one
CAS Number
170729-80-3
Synonyms
  • Emend
  • L-754,030
  • MK-869
  • ONO-7436
Molecular Formula
C23H21F7N4O3
Formula Weight
534.4
Purity
≥98%
Formulation (Request formulation change)
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
λmax
264, 271 nm
SMILES
C[C@@H](O[C@@H]1[C@H](C2=CC=C(F)C=C2)N(CC(NN3)=NC3=O)CCO1)C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4
InChi Code
InChI=1S/C23H21F7N4O3/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)37-20-19(13-2-4-17(24)5-3-13)34(6-7-36-20)11-18-31-21(35)33-32-18/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H2,31,32,33,35)/t12-,19+,20-/m1/s1
InChi Key
ATALOFNDEOCMKK-OITMNORJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $41

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    5 mg

    $90

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    10 mg

    $119

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    25 mg

    $196

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    Product Description

    Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM; IC50 = 0.09 nM for the human receptor).1,2 It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3).1 In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P (Item No. 24035).3 It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant 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

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