A peptide vasoconstrictor
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Endothelin-1 (human, porcine) (trifluoroacetate salt)

Item No. 24127

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Synonyms
  • ET-1
Molecular Formula
C109H159N25O32S5 • XCF3COOH
Formula Weight
2491.9
Purity
≥95%
Formulation (Request formulation change)
A lyophilized powder
Solubility(Learn about Variance in Solubility)
Formic Acid: 1 mg/ml
SMILES
OC([C@H](CC1=CNC2=C1C=CC=C2)NC([C@@]([H])(NC([C@@]([H])(NC([C@@H](NC([C@@H](NC([C@H](CC3=CNC=N3)NC([C@@H](NC([C@H](CC4=CC=CC=C4)NC([C@H](CC5=CC=C(C=C5)O)NC([C@H](C(C)C)NC([C@]6(NC([C@H](CCC(O)=O)NC([C@H](CCCCN)NC([C@H](CC(O)=O)NC7=O)=O)=O)=O)[H])=O)=O)=O)=O)CSSC[C@H](N)C(N[C@@H](CO)C(N[C@](C(N[C@@H](CO)C(N[C@@H](CO)C(N[C@@H](CC(C)C)C(N[C@H]7CCSC)=O)=O)=O)=O)(CSSC6)[H])=O)=O)=O)=O)CC(C)C)=O)CC(O)=O)=O)[C@H](CC)C)=O)[C@H](CC)C)=O)=O.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C109H159N25O32S5.C2HF3O2/c1-12-56(9)87(107(163)125-76(109(165)166)39-60-43-113-65-24-18-17-23-63(60)65)134-108(164)88(57(10)13-2)133-99(155)75(42-85(143)144)123-94(150)70(36-54(5)6)118-97(153)73(40-61-44-112-52-114-61)121-103(159)80-49-169-168-48-64(111)89(145)126-77(45-135)102(158)131-81-50-170-171-51-82(105(161)132-86(55(7)8)106(162)124-72(38-59-26-28-62(138)29-27-59)95(151)120-71(96(152)130-80)37-58-21-15-14-16-22-58)129-91(147)67(30-31-83(139)140)116-90(146)66(25-19-20-33-110)115-98(154)74(41-84(141)142)122-92(148)68(32-34-167-11)117-93(149)69(35-53(3)4)119-100(156)78(46-136)127-101(157)79(47-137)128-104(81)160;3-2(4,5)1(6)7/h14-18,21-24,26-29,43-44,52-57,64,66-82,86-88,113,135-138H,12-13,19-20,25,30-42,45-51,110-111H2,1-11H3,(H,112,114)(H,115,154)(H,116,146)(H,117,149)(H,118,153)(H,119,156)(H,120,151)(H,121,159)(H,122,148)(H,123,150)(H,124,162)(H,125,163)(H,126,145)(H,127,157)(H,128,160)(H,129,147)(H,130,152)(H,131,158)(H,132,161)(H,133,155)(H,134,164)(H,139,140)(H,141,142)(H,143,144)(H,165,166);(H,6,7)/t56-,57-,64-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,86-,87-,88-;/m0./s1
InChi Key
QJKWEQKXLNQIEY-GUNNUMSISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $415

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    1 mg

    $744

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    Cayman Chemical
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    Product Description

    Endothelin-1 is a peptide vasoconstrictor and agonist of endothelin (ET) receptors ETA and ETB (IC50s = 0.15 and 0.12 nM, respectively).1,2 It induces contraction of pig coronary artery strips (EC50 = 0.52 nM), vasoconstriction of pig cardiac ventricular membrane (120% of control), and increases mean early pressor phase blood pressure by 66 mg Hg in rats when administered at a dose of 1 nmol/kg. In an inducible system of endothelium-restricted overexpression of human endothelin-1, induction of endothelin-1 increases blood pressure in mice.3 It stabilizes and induces nuclear translocation of hypoxia-inducible factor 1 and 2 alpha (HIF-1α and HIF-2α) via ETB in human lymphatic endothelial cells.4 Endothelin-1 autocrine and paracrine signaling modulates cell proliferation, apoptosis, migration, and epithelial-to-mesenchymal transition, suggesting a role in cancer.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Inoue, A.Y., M., Kimura, S., Kasuya, Y., et al. The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc. Natl. Acad. Sci. USA 86(8), 2863-2867 (1989).

    2. Kikuchi, T., Kubo, K., Ohtaki, T., et al. Endothelin-1 analogues substituted at both position 18 and 19: Highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB. J. Med. Chem. 36(25), 4087-4093 (1993).

    3. Rautureau, Y., Coelho, S.C., Fraulob-Aquino, J.C., et al. Inducible human endothelin-1 overexpression in endothelium raises blood pressure via endothelin type A receptors. Hypertension 66(2), 347-355 (2015).

    4. Caprara, V., Scappa, S., Garrafa, E., et al. Endothelin-1 regulates hypoxia-inducible factor-1α and -2α stability through prolyl hydroxylase domain 2 inhibition in human lymphatic endothelial cells. Life Sci. 118(2), 185-190 (2014).

    5. Rosanò, L., Spinella, F., and Bagnato, A. Endothelin 1 in cancer: Biological implications and therapeutic opportunities. Nat. Rev. Cancer 13(9), 637-651 (2013).