A GRP/bombesin receptor 2 antagonist
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ICI 216140 (trifluoroacetate salt)

Item No. 17479

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-methyl-1-oxopropyl)-7-D-alanine-9-(N-methyl-L-leucinamide)-3-9-neuromedin C, trifluoroacetate salt
Molecular Formula
C45H65N13O8 • XCF3COOH
Formula Weight
916.1
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
218, 280, 290 nm
SMILES
CC(C)C(N[C@@H](CC1=CNC=N1)C(N[C@@H](CC2=CNC3=C2C=CC=C3)C(N[C@@H](C)C(N[C@@H](C(C)C)C(N[C@H](C)C(N[C@@H](CC4=CNC=N4)C(N[C@@H](CC(C)C)C(NC)=O)=O)=O)=O)=O)=O)=O)=O.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C45H65N13O8.C2HF3O2/c1-23(2)14-33(41(62)46-9)56-44(65)36(17-30-20-48-22-51-30)55-39(60)26(7)53-45(66)37(24(3)4)58-40(61)27(8)52-42(63)34(15-28-18-49-32-13-11-10-12-31(28)32)57-43(64)35(54-38(59)25(5)6)16-29-19-47-21-50-29;3-2(4,5)1(6)7/h10-13,18-27,33-37,49H,14-17H2,1-9H3,(H,46,62)(H,47,50)(H,48,51)(H,52,63)(H,53,66)(H,54,59)(H,55,60)(H,56,65)(H,57,64)(H,58,61);(H,6,7)/t26-,27+,33+,34+,35+,36+,37+;/m1./s1
InChi Key
XYCOOCFLZFLEPC-KQCGLQBDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $169

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    1 mg

    $303

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    5 mg

    $835

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    Product Description

    ICI 216140 is a GRP/bombesin receptor 2 antagonist (IC50 = 2 nM in vitro).1 At 2 mg/kg, it can reduce bombesin-stimulated pancreatic amylase secretion in rats.1 At 1 mM, it has been shown to attenuate bombesin-stimulated increases in blood pressure in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Camble, R., Cotton, R., Dutta, A.S., et al. N-isobutyryl-His-Trp-Ala-Val-D-Ala-His-Leu-NHMe (ICI 216140) a potent in vivo antagonist analogue of bombesin/gastrin releasing peptide (BN/GRP) derived from the C-terminal sequence lacking the final methionine residue. Life Sci. 45(17), 1521-1527 (1989).

    2. Zogovic, B., and Pilowsky, P.M. Intrathecal bombesin is sympathoexcitatory and pressor in rat. Am. J. Physiol. Regul. Integr. Comp. Physiol. 301(5), R1486-R1494 (2011).