A peptide antagonist of NK1 and NK2 receptors
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Spantide II (trifluoroacetate salt)

Item No. 43054

Technical Information
Formal Name
N6-(3-pyridinylcarbonyl)-D-lysyl-L-prolyl-3-(3-pyridinyl)-L-alanyl-L-prolyl-3,4-dichloro-D-phenylalanyl-L-asparaginyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-L-leucyl-L-norleucinamide
Synonyms
  • [D-NicLys1,3-Pal3,D-Cl2Phe5,Asn6,D-Trp7,9,Nle11]-Substance P
Molecular Formula
C86H104Cl2N18O13 • XCF3COOH
Formula Weight
Purity
≥98%
A solid
Peptide Sequence
x1PX2Px3NwFwLX4-NH2 (X1 = N6-(nicotinyl)-D-lysine; X2 = 3-pyri
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(N[C@H](CC1=CNC2=CC=CC=C21)C(N[C@H](C(N[C@H](CC3=CNC4=CC=CC=C43)C(N[C@H](C(N[C@@H](CCCC)C(N)=O)=O)CC(C)C)=O)=O)CC5=CC=CC=C5)=O)[C@@H](NC([C@@H](CC6=CC(Cl)=C(Cl)C=C6)NC([C@@H]7CCCN7C([C@@H](NC([C@@H]8CCCN8C([C@@H](CCCCNC(C9=CN=CC=C9)=O)N)=O)=O)CC%10=CN=CC=C%10)=O)=O)=O)CC(N)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C86H104Cl2N18O13.C2HF3O2/c1-4-5-26-64(75(91)108)97-77(110)65(38-50(2)3)98-80(113)68(43-55-48-95-62-27-11-9-23-57(55)62)100-78(111)66(40-51-19-7-6-8-20-51)99-81(114)69(44-56-49-96-63-28-12-10-24-58(56)63)101-82(115)70(45-74(90)107)102-79(112)67(41-52-31-32-59(87)60(88)39-52)103-83(116)73-30-18-37-106(73)86(119)71(42-53-21-15-33-92-46-53)104-84(117)72-29-17-36-105(72)85(118)61(89)25-13-14-35-94-76(109)54-22-16-34-93-47-54;3-2(4,5)1(6)7/h6-12,15-16,19-24,27-28,31-34,39,46-50,61,64-73,95-96H,4-5,13-14,17-18,25-26,29-30,35-38,40-45,89H2,1-3H3,(H2,90,107)(H2,91,108)(H,94,109)(H,97,110)(H,98,113)(H,99,114)(H,100,111)(H,101,115)(H,102,112)(H,103,116)(H,104,117);(H,6,7)/t61-,64+,65+,66+,67-,68-,69-,70+,71+,72+,73+;/m1./s1
InChi Key
MZHYSCPSSYIQPF-SJPYZGNSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Spantide II is a peptide neurokinin-1 (NK1) and NK2 receptor antagonist (Kis = 2.4 and 19.05 nM, respectively).1 It induces histamine release from isolated rat mast cells (EC50 = 3.2 µM).2 Spantide II (10 µM) inhibits bombesin-induced contractions in isolated and perfused guinea pig taenia coli when used at a concentration of 10 µM. Topical application of spantide II (0.05-1% (w/v) three times per day) decreases ear swelling in a mouse model of allergic contact dermatitis induced by 2,4-dinitro-1-fluorobenzene.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Janecka, A., Poels, J., Fichna, J., et alComparison of antagonist activity of spantide family at human neurokinin receptors measured by aequorin luminescence-based functional calcium assay. Regul. Pept. 131(1-3), 23-28 (2005).

    2. McLean, S., Ganong, A., Seymour, P.A., et alPharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J. Pharmacol. Exp. Ther. 267(1), 472-479 (1993).

    3. Kikwai, L., Babu, R.J., Prado, R., et alIn vitro and in vivo evaluation of topical formulations of spantide II. AAPS PharmSciTech 6(4), E565-E572 (2005).