A peptide ETB receptor antagonist
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Alternative(s)
31156BQ-788
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BQ-788 (sodium salt)

Item No. 17403

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine, monosodium salt
CAS Number
156161-89-6
Molecular Formula
C34H51N5O7 • Na
Formula Weight
664.8
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
229, 258, 286, 294 nm
SMILES
C[C@H]1N([C@H](CCC1)C)C(N[C@H](C(N[C@H](CC2=CN(C3=C2C=CC=C3)C(OC)=O)C(N[C@H](CCCC)C(O)=O)=O)=O)CC(C)(C)C)=O.[Na]
InChi Code
InChI=1S/C34H51N5O7.Na/c1-8-9-16-25(31(42)43)35-29(40)26(18-23-20-38(33(45)46-7)28-17-11-10-15-24(23)28)36-30(41)27(19-34(4,5)6)37-32(44)39-21(2)13-12-14-22(39)3;/h10-11,15,17,20-22,25-27H,8-9,12-14,16,18-19H2,1-7H3,(H,35,40)(H,36,41)(H,37,44)(H,42,4
InChi Key
IASLQTYUGYPLFB-FUKQNADPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Cayman Chemical
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    Product Description

    BQ-788 is a peptide endothelin type B (ETB) receptor antagonist (IC50 = 1.2 nM).1 It is selective for ETB over ETA receptors (IC50 = 280 nM), as well as angiotensin, calcitonin, or neuropeptide receptors at 10 µM. BQ-788 inhibits calcium mobilization induced by endothelin-1 (ET-1) in human Girrardi heart cells (IC50 = 0.54 nM) and vasoconstriction induced by the ETB-selective agonist BQ-3020 in isolated rat pulmonary arteries (pA2 = 8.4).2 In vivo, BQ-788 (1 mg/kg, i.v.) inhibits ET-1-induced depressor responses and induces pressor responses in rats. It protects against laparotomy and surgical gut handling-induced inhibition of intestinal motility in rats.3 BQ-788 also attenuates delayed hypotension, vascular hyporeactivity to norepinephrine, and hepatocellular injury and dysfunction in a rat model of LPS-induced endotoxemia.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Okada, M., and Nishikibe, M. BQ-788, a selective endothelin ETB receptor antagonist. Cardiovasc. Drug Rev. 20(1), 53-66 (2002).

    2. Ishikawa, K., Ihara, M., Noguchi, K., et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl. Acad. Sci. USA 91(11), 4892-4896 (1994).

    3. Ługowska-Umer, H., Umer, A., Kuziemski, K., et al. The protective effect of endothelin receptor antagonists against surgically induced impairment of gastrointestinal motility in rats. J. Smooth Muscle Res. 55, 23-33 (2019).

    4. Ruetten, H., and Thiemermann, C. Effect of selective blockade of endothelin ETB receptors on the liver dysfunction and injury caused by endotoxaemia in the rat. Br. J. Pharmacol. 119(3), 479-486 (1996).