An endogenous agonist of the APJ receptor
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Apelin-12 (human, mouse, rat, bovine) (acetate)

Item No. 36888

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-seryl-L-histidyl-L-lysylglycyl-L-prolyl-L-methionyl-L-prolyl-L-phenylalanine, acetate
Synonyms
  • RPRLSHKGPMPF
Molecular Formula
C64H103N21O14S • XC2H4O2
Formula Weight
1422.7
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: insolDMSO: insolEthanol: insolPBS (pH 7.2): 5 mg/ml
SMILES
O=C([C@H]1N(CCC1)C(CNC([C@H](CCCCN)NC([C@@H](NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CCCNC(N)=N)NC([C@H]2N(CCC2)C([C@@H](N)CCCNC(N)=N)=O)=O)=O)=O)=O)CC3=CN=CN3)=O)=O)=O)N[C@@H](CCSC)C(N4[C@@H](CCC4)C(N[C@H](C(O)=O)CC5=CC=CC=C5)=O)=O.CC(O)=O
InChi Code
InChI=1S/C64H103N21O14S.C2H4O2/c1-37(2)30-44(79-53(89)42(18-10-25-73-64(69)70)77-58(94)49-20-12-27-84(49)60(96)40(66)16-9-24-72-63(67)68)54(90)82-47(35-86)56(92)80-45(32-39-33-71-36-75-39)55(91)76-41(17-7-8-23-65)52(88)74-34-51(87)83-26-11-19-48(83)57(93)78-43(22-29-100-3)61(97)85-28-13-21-50(85)59(95)81-46(62(98)99)31-38-14-5-4-6-15-38;1-2(3)4/h4-6,14-15,33,36-37,40-50,86H,7-13,16-32,34-35,65-66H2,1-3H3,(H,71,75)(H,74,88)(H,76,91)(H,77,94)(H,78,93)(H,79,89)(H,80,92)(H,81,95)(H,82,90)(H,98,99)(H4,67,68,72)(H4,69,70,73);1H3,(H,3,4)/t40-,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-;/m0./s1
InChi Key
PWUOUGMQUHCVDK-SBNCYDFUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Apelin-12 is a 12-amino acid peptide fragment corresponding to residues 66-77 of apelin and an endogenous agonist of the apelin receptor (APJ), with roles in viral immunity, digestion, cell cycle regulation, and vasodilation.1 It induces calcium mobilization in APJ-Gαq16 cells expressing human APJ (EC50 = 0.18 nM). Apelin-12 inhibits HIV-1 and HIV-2 infection in NP-2/CD4/APJ cells (mean IC50 = 63 µg/ml).2 It inhibits or stimulates the expression of genes associated with apoptosis, mitosis, and DNA repair in IEC-6 and Caco-2 cells, respectively, when used at a concentration of 0.01 µM.3 Apelin-12 (100-1,000 nM) induces the production of nitric oxide (NO) via PI3K and Akt signaling pathways in human umbilical vein endothelial cells (HUVECs).4 In vivo, apelin-12 (20-100 µg/kg) increases gastric acid secretion, as well as stomach histamine synthesis and secretion, in rats.5 It also reduces mean arterial pressure (MAP) in rats when administered at a dose of 15 µg/kg.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Giddings, A., Runyon, S., Thomas, J., et al. Development of a functional HTS assay for the APJ receptor. Int. J. High Throughput Screen. 1, 39-47 (2010).

    2. Zou, M.X., Liu, H.Y., Haraguchi, Y., et al. Apelin peptides block the entry of human immunodeficiency virus (HIV). FEBS Lett. 473(1), 15-18 (2000).

    3. Antushevich, H., Krawczynska, A., Kapica, M., et al. Effect of apelin on mitosis, apoptosis and DNA repair enzyme OGG ½ expression in intestinal cell lines IEC-6 and Caco-2. Folia Histochem. Cytobiol. 52(1), 51-59 (2014).

    4. Busch, R., Strohbach, A., Pennewitz, M., et al. Regulation of the endothelial apelin/APJ system by hemodynamic fluid flow. Cell. Signal. 27(7), 1286-1296 (2015).

    5. Ohno, S., Yakabi, K., Ro, S., et al. Apelin-12 stimulates acid secretion through an increase of histamine release in rat stomachs. Regul. Pept. 174(1-3), 71-79 (2012).

    6. Lee, D.K., Saldivia, V.R., Nguyen, T., et al. Modification of the terminal residue of apelin-13 antagonizes its hypotensive action. Endocrinology 146(1), 231-236 (2005).