A peptide antagonist of the NK1 receptor
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Physalaemin (frog) (trifluoroacetate salt)

Item No. 43045

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-5-oxo-L-prolyl-L-alanyl-L-aspartyl-L-prolyl-L-asparaginyl-L-lysyl-L-phenylalanyl-L-tyrosylglycyl-L-leucyl-methioninamide, trifluoroacetate salt
CAS Number
4705-64-0
Molecular Formula
C58H84N14O16S • XCF3COOH
Formula Weight
1265.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Peptide Sequence
XADPNKFYGLM-NH2 (X = Pyroglutamic acid)
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/mlPBS (pH 7.2): Soluble: ≥ 10 mg/ml
SMILES
NC(C[C@H](NC([C@H]1N(C([C@@H](NC([C@H](C)NC([C@@H]2CCC(N2)=O)=O)=O)CC(O)=O)=O)CCC1)=O)C(N[C@H](C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CC4=CC=C(O)C=C4)C(NCC(N[C@H](C(N[C@@H](CCSC)C(N)=O)=O)CC(C)C)=O)=O)=O)=O)CCCCN)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C58H84N14O16S.C2HF3O2/c1-31(2)25-39(54(84)66-36(49(61)79)21-24-89-4)65-47(76)30-62-51(81)40(27-34-15-17-35(73)18-16-34)68-55(85)41(26-33-11-6-5-7-12-33)69-53(83)37(13-8-9-22-59)67-56(86)42(28-45(60)74)70-57(87)44-14-10-23-72(44)58(88)43(29-48(77)78)71-50(80)32(3)63-52(82)38-19-20-46(75)64-38;3-2(4,5)1(6)7/h5-7,11-12,15-18,31-32,36-44,73H,8-10,13-14,19-30,59H2,1-4H3,(H2,60,74)(H2,61,79)(H,62,81)(H,63,82)(H,64,75)(H,65,76)(H,66,84)(H,67,86)(H,68,85)(H,69,83)(H,70,87)(H,71,80)(H,77,78);(H,6,7)/t32-,36-,37-,38-,39-,40-,41-,42-,43-,44-;/m0./s1
InChi Key
DDNSQNUDDOKWMI-FKIDJSLMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $83

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    5 mg

    $351

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    10 mg

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    25 mg

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    Product Description

    Physalaemin is a peptide antagonist of the neurokinin-1 (NK1) receptor (Ki = 1.51 nM).1 It is selective for the NK1 receptor over the NK3 receptor (Ki = 457 nM). Physalaemin (2.5 µM) increases the percentage of cell clusters displaying neurite outgrowth and inhibits toxicity induced by amyloid-β peptides in NB41A3 cells.2 It induces contraction in isolated and perfused guinea pig taenia coli when used at a concentration of 1 µM.3 In vivo, physalaemin (2 µg/kg) decreases arterial blood pressure and induces salivation in normotensive dogs.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Antoniou, M., and Poulos, C. Analogues of the C-terminal fragments of neurokinins with modifications at their C-terminal methionyl residue. Structure-activity studies. Int. J. Pept. Protein Res. 43(4), 344-350 (1994).

    2. Zhao, X., Valantas, J.A., Vyas, S., et al. Comparative toxicity of amyloid β-peptide in neuroblastoma cell lines: Effects of albumin and physalaemin. Comp. Biochem. Physiol. C Comp. Pharmacol. Toxicol. 106(1), 165-170 (1993).

    3. Leander, S., Håkanson, R., Rosell, S., et al. A specific substance P antagonist blocks smooth muscle contractions induced by non-cholinergic, non-adrenergic nerve stimulation. Nature 294(5840), 467-469 (1981).

    4. Bertaccini, G., and De Caro, G. The effect of physalaemin and related polypeptides on salivary secretion. J. Physiol. 181(1), 68-81 (1965).