An NK1 receptor antagonist
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L-732,138

Item No. 30894

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-acetyl-L-tryptophan [3,5-bis(trifluoromethyl)phenyl]methyl ester
CAS Number
148451-96-1
Molecular Formula
C22H18F6N2O3
Formula Weight
472.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
221 nm
SMILES
CC(N[C@@H](CC1=CNC2=C1C=CC=C2)C(OCC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)=O
InChi Code
InChI=1S/C22H18F6N2O3/c1-12(31)30-19(8-14-10-29-18-5-3-2-4-17(14)18)20(32)33-11-13-6-15(21(23,24)25)9-16(7-13)22(26,27)28/h2-7,9-10,19,29H,8,11H2,1H3,(H,30,31)/t19-/m0/s1
InChi Key
BYYQYXVAWXAYQC-IBGZPJMESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $69

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    10 mg

    $120

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    50 mg

    $461

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    100 mg

    $852

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    Cayman Chemical
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    Product Description

    L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor).1 It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines.2 It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.).1 L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. MacLeod, A.M., Merchant, K.J., Brookfield, F., et al. Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. J. Med. Chem. 37(9), 1269-1274 (1994).

    2. Muñoz, M., Rosso, M., González-Ortega, A., et al. The NK-1 receptor antagonist L-732,138 induces apoptosis and counteracts substance P-related mitogenesis in human melanoma cell lines. Cancers (Basel) 2(2), 611-623 (2010).

    3. Cahill, C.M., and Coderre, T.J. Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre- or post-treatment with a neurokinin-1 antagonist. Pain 95(3), 277-285 (2002).