A peptide inhibitor of K2P2.1/TREK1
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PE 22-28 (acetate)

Item No. 39986

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
glycyl-L-valyl-L-seryl-L-tryptophylglycyl-L-leucyl-L-arginine, acetate
Synonyms
  • Gly-Val-Ser-Trp-Gly-Leu-Arg-OH
Molecular Formula
C35H55N11O9 • XC2H4O2
Formula Weight
773.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Peptide Sequence
GVSWGLR-OH
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleMethanol: Soluble
SMILES
O=C(NCC(N[C@@H](CC(C)C)C(N[C@H](C(O)=O)CCCNC(N)=N)=O)=O)[C@@H](NC([C@H](CO)NC([C@H](C(C)C)NC(CN)=O)=O)=O)CC1=CNC2=CC=CC=C12.OC(C)=O
InChi Code
InChI=1S/C35H55N11O9.C2H4O2/c1-18(2)12-24(31(51)43-23(34(54)55)10-7-11-39-35(37)38)42-28(49)16-41-30(50)25(13-20-15-40-22-9-6-5-8-21(20)22)44-32(52)26(17-47)45-33(53)29(19(3)4)46-27(48)14-36;1-2(3)4/h5-6,8-9,15,18-19,23-26,29,40,47H,7,10-14,16-17,36H2,1-4H3,(H,41,50)(H,42,49)(H,43,51)(H,44,52)(H,45,53)(H,46,48)(H,54,55)(H4,37,38,39);1H3,(H,3,4)/t23-,24-,25-,26-,29-;/m0./s1
InChi Key
BALNOYNMJOOJJD-GVRVQHEFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $98

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    1 mg

    $186

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    5 mg

    $490

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    Product Description

    PE 22-28 is a peptide inhibitor of the two-pore domain potassium channel K2P2.1/TREK1 (IC50 = 0.1 nM in HEK293 cells expressing the human channel) and a fragment of spadin (Item No. 36762).1 It is selective for K2P2.1/TREK1 over K2P10.1 /TREK2, K2P13.1/TRAAK, K2P18.1/TRESK, and K2P3.1/TASK1 in HEK293 cells expressing the human channels at 100 nM. PE 22-28 (4 µg/kg for four days) increases neurogenesis and the levels of postsynaptic density protein 95 (Psd-95), a measure of increased synaptogenesis, in isolated mouse hippocampi. It decreases immobility in the forced swim test, latency to feed in the novelty-suppressed feeding test, and the time to escape in the Porsolt learned helplessness test in mice when administered at a dose of 0.3 µg/kg for four days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Djillani, A., Pietri, M., Moreno, S., et al. Shortened spadin analogs display better TREK-1 inhibition, in vivo stability and antidepressant activity. Front. Pharmacol. 8:643, (2017).