A peptide ETB receptor antagonist
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BQ-3020 (trifluoroacetate salt)

Item No. 34014

Technical Information
Formal Name
N-acetyl-11-L-alanine-15-L-alanine-6-21-endothelin 1 (swine reduced), trifluoroacetate salt
Molecular Formula
C96H140N20O25S • XCF3COOH
Formula Weight
Purity
≥90%
A solid
DMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
OC(C=C1)=CC=C1C[C@H](NC([C@H](C(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](CCCCN)NC([C@H](CC(O)=O)NC([C@H](CCSC)NC([C@@H](NC(C)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](C)C(N[C@@H](CC3=CN=CN3)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(O)=O)CC4=CNC5=CC=CC=C45)=O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C96H140N20O25S.C2HF3O2/c1-15-52(9)79(94(138)113-74(96(140)141)42-59-46-99-63-27-21-20-26-62(59)63)116-95(139)80(53(10)16-2)115-92(136)73(45-77(123)124)111-88(132)68(39-50(5)6)108-90(134)71(43-60-47-98-48-100-60)107-81(125)54(11)102-86(130)69(40-57-24-18-17-19-25-57)109-89(133)70(41-58-29-31-61(118)32-30-58)112-93(137)78(51(7)8)114-82(126)55(12)101-83(127)65(33-34-75(119)120)105-84(128)64(28-22-23-36-97)104-91(135)72(44-76(121)122)110-85(129)66(35-37-142-14)106-87(131)67(38-49(3)4)103-56(13)117;3-2(4,5)1(6)7/h17-21,24-27,29-32,46-55,64-74,78-80,99,118H,15-16,22-23,28,33-45,97H2,1-14H3,(H,98,100)(H,101,127)(H,102,130)(H,103,117)(H,104,135)(H,105,128)(H,106,131)(H,107,125)(H,108,134)(H,109,133)(H,110,129)(H,111,132)(H,112,137)(H,113,138)(H,114,126)(H,115,136)(H,116,139)(H,119,120)(H,121,122)(H,123,124)(H,140,141);(H,6,7)/t52-,53-,54-,55-,64-,65-,66-,67-,68-,69-,70-,71-,72-,73-,74-,78-,79-,80-;/m0./s1
InChi Key
GKAQAMTYCWGAFR-IRZCQVHSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    BQ-3020 is a peptide endothelin type B (ETB) receptor agonist.1 It selectively binds to ETB over ETA receptors (IC50s = 0.07 and 940 nM, respectively) and induces inositol triphosphate formation and calcium mobilization in isolated bovine carotid artery endothelial cells.1,2 BQ-3020 increases or decreases renal perfusion pressure in Dahl salt-resistant or -sensitive rats, respectively.3 It decreases the production of nitric oxide (NO) and induces vasoconstriction in a rat model of diet-induced hypercholesterolemia.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ihara, M., Saek, T., Fukuroda, T., et alA novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 51(6), PL47-PL52 (1992).

    2. Hirata, Y., Emori, T., Eguchi, S., et alEndothelin receptor subtype B mediates synthesis of nitric oxide by cultured bovine endothelial cells. J. Clin. Invest. 91(4), 1367-1373 (1993).

    3. Kakoki, M., Hirata, Y., Hayakawa, H., et alEffects of hypertension, diabetes mellitus, and hypercholesterolemia on endothelin type B receptor-mediated nitric oxide release from rat kidney. Circulation 99(9), 1242-1248 (1999).