A peptide antagonist of APJ
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MM-54 (trifluoroacetate salt)

Item No. 42401

Technical Information
Formal Name
L-cysteinyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-cysteinyl-L-lysyl-L-histidyl-L-cysteinyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-cysteine, cyclic (1→6),(9→14)-bis(disulfide), trifluoroacetate salt
Molecular Formula
C70H121N29O15S4 • XCF3COOH
Formula Weight
Purity
≥95%
A solid
Peptide Sequence
cyclic[CRPRLC]-KH-cyclic[CRPRLC]-OH
DMSO: Sparingly Soluble: 1-10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/mlPBS (pH 7.2): Sparingly Soluble: 1-10 mg/ml
SMILES
O=C1N2[C@@](C(N[C@H](C(N[C@H](C(N[C@@H](CSSC[C@@H](C(N[C@H]1CCCNC(N)=N)=O)NC([C@@H](NC([C@H](CCCCN)NC([C@H]3NC([C@@H](NC([C@@H](NC([C@@]4([H])N(CCC4)C([C@@H](NC([C@H](CSSC3)N)=O)CCCNC(N)=N)=O)=O)CCCNC(N)=N)=O)CC(C)C)=O)=O)=O)CC5=CN=CN5)=O)C(O)=O)=O)CC(C)C)=O)CCCNC(N)=N)=O)([H])CCC2.FC(F)(F)C(O)=O
InChi Code
InChI=1S/C70H121N29O15S4.C2HF3O2/c1-36(2)27-45-57(104)95-48(32-116-115-31-39(72)53(100)90-43(16-9-23-84-69(77)78)64(111)98-25-11-18-51(98)62(109)88-41(55(102)92-45)14-7-21-82-67(73)74)60(107)87-40(13-5-6-20-71)54(101)94-47(29-38-30-81-35-86-38)59(106)96-49-33-117-118-34-50(66(113)114)97-58(105)46(28-37(3)4)93-56(103)42(15-8-22-83-68(75)76)89-63(110)52-19-12-26-99(52)65(112)44(91-61(49)108)17-10-24-85-70(79)80;3-2(4,5)1(6)7/h30,35-37,39-52H,5-29,31-34,71-72H2,1-4H3,(H,81,86)(H,87,107)(H,88,109)(H,89,110)(H,90,100)(H,91,108)(H,92,102)(H,93,103)(H,94,101)(H,95,104)(H,96,106)(H,97,105)(H,113,114)(H4,73,74,82)(H4,75,76,83)(H4,77,78,84)(H4,79,80,85);(H,6,7)/t39-,40-,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-;/m0./s1
InChi Key
KTMDLQYXMOBVMO-QRIILVICSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MM-54 is a peptide antagonist of the apelin receptor (APJ; Ki = 82 nM).1 It inhibits apelin-13-induced increases in number of stem cells and tumorspheres and the percentage of cells with aldehyde dehydrogenase (ALDH) activity, a marker of stem cells, in patient-derived glioblastoma spheroids when used at a concentration of 100 µM.2 MM-54 (2 mg/kg twice per week) decreases tumor volume in a patient-derived xenograft (PDX) mouse model of glioblastoma.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Macaluso, N.J., Pitkin, S.L., Maguire, J.J., et alDiscovery of a competitive apelin receptor (APJ) antagonist. ChemMedChem 6(6), 1017-1023 (2011).

    2. Harford-Wright, E., Andre-Gregoire, G., Jacobs, K.A., et alPharmacological targeting of apelin impairs glioblastoma growth. Brain 40(11), 2939-2954 (2017).