Antagonists

Endothelin

The vascular response to infusion of endothelin-1 shows a short relaxation of tone followed by long-lasting constriction. 1 Receptor specific antagonists like BQ-123 and PD-156707(specific to ETA receptors) and BQ-788 (specific to ETB receptors) have shown that binding to ETA primarily promotes vascular smooth muscle contraction and endothelial cell proliferation. Binding of endothelin-1 to ETB receptors results in NO release that causes short-term smooth muscle relaxation. The ETB receptor is also responsible for clearing endothelin-1 from the circulation.2 The endothelins participate in many non-circulatory systems, so that antagonists may have multiple effects. For example, the antibiotic kendamycin is a strong endothelin receptor antagonist that also has antiosteoporotic activity and seems to affect protein turnover by the ubiquitin system. Sitaxentan, an ETA antagonist, seemed to be a promising treatment for pulmonary arterial hypertension, but was toxic to the liver. Development of endothelin antagonists is an active area in drug development.

1. Inoue, A. et al. Proc. Natl. Acad. Sci., USA 86:2863 (1989)
2. Endothelin Receptors, Sigma publication.

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116765 Adenosine A 2A/A₁ Receptor Antagonist - Calbiochem The Adenosine A2A/A₁ Receptor Antagonist controls the biological activity of Adenosine A2A/A₁ Receptor. This small molecule/inhibitor is primarily used for Biochemicals applications.  
1191 Adenosine 5ʹ-Triphosphate, Disodium Salt - CAS 987-65-5 - Calbiochem  
182707 AhR Antagonist III, GNF351 - Calbiochem AhR Antagonist III, GNF351, is a cell-permeable, high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR).  
165304 D-(–)-2-Amino-5-phosphonopentanoic Acid - CAS 79055-68-8 - Calbiochem Active enantiomer of DL-2-amino-5-phosphonopentanoic acid (AP5) that is a commonly used as a competitive NMDA receptor antagonist. Cell permeable: no
Primary Target
NMDA receptor antagonist
Product does not compete with ATP.
Reversible: no
178477 ApoE4 Modulator, PH002 - Calbiochem A phthalazinone derived compound that directly binds to the 22-kDa amino-terminal region of apolipoprotein E4 (ApoE4) and blocks its intramolecular domain interactions in neuronal cells thereby reversing the detrimental effects of ApoE4. Cell permeable: yes
Primary Target
APOE4
Reversible: yes
SML0708 BMS-182874 hydrochloride ≥98% (HPLC) BMS-182874 is a potent selective nonpeptide endothelin ETA receptor antagonist. BMS-182874 is 1000-fold selective for ETA over ETA B receptors with a Ki of 48 nM for ETA receptors vs >50 μM for ETB.
BM0014 BMS-207940 ≥98% (HPLC) BMS-207940 is a very potent and selective ETA endothelin receptor antagonist. BMS-207940 has a Ki of 10 pM for ETA, 80000-fold selective for ETA vs ETB.
SML1265 Bosentan hydrate ≥98% (HPLC) Bosentan is an endothelin receptor antagonist. Endothelin is a potent vasoconstrictor, making antagonists of clinical interest for the treatment of conditions associated with vasospasm, such as subarachnoid hemorrhage (SAH) and hypertension. Bosentan is a dual endothelin receptor antagonist effective in the treatment of pulmonary arterial hypertension (PAH), the first of the class to make it to market. Bosentan is an orally available, competitive antagonist of both the ETA and ETB receptor subtypes with a Ki of 4.7 nM for ETA and a Ki of 95 nM for ETB.
Bosentan is found to decrease deposition of collagen in the lungs, which has been observed in bleomycin-induced pulmonary fibrosis rat model.
B150 BQ-123 ≥99%, sodium salt, lyophilized powder Selective ETA endothelin receptor antagonist.
203715 BQ-610 - Calbiochem A highly selective ETA receptor antagonist (IC₅₀ = 20 nM) that attenuates ET-induced reduction in cardiac output. Cell permeable: no
Primary Target
ETA receptor antagonist
Product does not compete with ATP.
Reversible: no
Target IC50: 20 nM as ETA receptor antagonist that attenuates ET-induced reduction in cardiac output
B157 BQ-788 ≥95%, solid Selective ETB endothelin receptor antagonist.
208735 Calmodulin Inhibitory Peptide - Calbiochem The Calmodulin Inhibitory Peptide controls the biological activity of Calmodulin. This small molecule/inhibitor is primarily used for Cell Signaling applications. Cell permeable: no
Kd = 6 pM in binding to calmodulin
Primary Target
Calmodulin
Product does not compete with ATP.
Reversible: no
208736 Calmodulin Inhibitory Peptide, Control - Calbiochem The Calmodulin Inhibitory Peptide, Control controls the biological activity of Calmodulin. This small molecule/inhibitor is primarily used for Cell Signaling applications. Cell permeable: no
Primary Target
A control peptide for Calmodulin Inhibitory Peptide (Cat. No. 208735)
Product does not compete with ATP.
Reversible: no
211280 Capsazepine - CAS 138977-28-3 - Calbiochem A competitive antagonist of Capsaicin and resiniferatoxin. Capsazepine (1 µM) blocks capsaicin (60 nM) stimulated firing of C-fibers. Cell permeable: no
Primary Target
A competitive antagonist of Capsaicin and resiniferatoxin
Product does not compete with ATP.
Reversible: no
239819 CXCR2 antagonist, Cpd 19 - CAS 473728-67-5 - Calbiochem The CXCR2 antagonist, Cpd 19, also referenced under CAS 473728-67-5, controls the biological activity of CXCR2.  
239820 CXCR4 Antagonist I, AMD3100 - CAS 155148-31-5 - Calbiochem The CXCR4 Antagonist I, AMD3100, also referenced under CAS 155148-31-5, controls the biological activity of CXCR4. This small molecule/inhibitor is primarily used for Cell Signaling applications.  
239821 CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem The CXCR4 Antagonist II, also referenced under CAS 1258011-83-4, controls the biological activity of CXCR4. This small molecule/inhibitor is primarily used for Cell Signaling applications.  
239822 CXCR4 Antagonist III - Calbiochem The CXCR4 Antagonist III controls the biological activity of CXCR4. This small molecule/inhibitor is primarily used for Biochemicals applications. Cell permeable: yes
Reversible: yes
324387 Dopamine Receptor Antagonist II, Thioridazine, HCl - CAS 130-61-0 - Calbiochem The Dopamine Receptor Antagonist II, Thioridazine, HCl, also referenced under CAS 130-61-0, controls the biological activity of Dopamine Receptor. This small molecule/inhibitor is primarily used for Biochemicals applications.  
344220 Formyl Peptide Receptor-Like 1 Antagonist, WRW⁴ - Calbiochem The Formyl Peptide Receptor-Like 1 Antagonist, WRW⁴ controls the biological activity of Formyl Peptide Receptor-Like 1. Cell permeable: no
Primary Target
Formyl Peptide Receptor-Like 1 (FPRL1)
Product does not compete with ATP.
Reversible: no
Target IC50: 230 nM for FPRL1 Agonist
362330 GAG Antagonist, Surfen - Calbiochem The GAG Antagonist, Surfen controls the biological activity of GAG. This small molecule/inhibitor is primarily used for Activators/Inducers applications.  
346003 Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem The Glucagon Receptor Antagonist II, also referenced under CAS 191034-25-0, controls the biological activity of Glucagon Receptor. Cell permeable: yes
Primary Target
Glucagon Receptor
Product does not compete with ATP.
Reversible: no
Target IC50: 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively
371780 GP Antagonist-2A - Calbiochem The GP Antagonist-2A controls the biological activity of GP. This small molecule/inhibitor is primarily used for Neuroscience applications. Cell permeable: no
Primary Target
Inhibits the activation of Gq by M1-muscarinic cholinergic receptors
Product does not compete with ATP.
Reversible: no
371830 GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem The GPR40 Antagonist, GW1100, also referenced under CAS 306974-70-9, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.  
373402 Hedgehog Antagonist VIII - CAS 330796-24-2 - Calbiochem The Hedgehog Antagonist VIII, also referenced under CAS 330796-24-2, controls the biological activity of Hedgehog. This small molecule/inhibitor is primarily used for Cell Signaling applications.  
373400 Hh/Gli Antagonist, GANT58 - CAS 64048-12-0 - Calbiochem The Hh/Gli Antagonist, GANT58, also referenced under CAS 64048-12-0, controls the biological activity of Hh/Gli. This small molecule/inhibitor is primarily used for Cell Signaling applications.  
375240 HNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem The HNF4 Antagonist, BI6, also referenced under CAS 93987-29-2, controls the biological activity of HNF4. Cell permeable: yes
Primary Target
HNFα & γ
Reversible: yes
407621 IL-2Rα Antagonist - CAS 1217448-66-2 - Calbiochem The IL-2Rα Antagonist, also referenced under CAS 1217448-66-2, controls the biological activity of IL-2Rα. Cell permeable: no
Primary Target
Inhibitor of the IL-2/IL-2Rα interaction
Product does not compete with ATP.
Reversible: no
Target IC50: 3 µM against IL-2/IL-2Rα interaction
407616 IL-1R Antagonist - CAS 566914-00-9 - Calbiochem The IL-1R Antagonist, also referenced under CAS 566914-00-9, controls the biological activity of IL-1R. Cell permeable: yes
Primary Target
TIR domain-mediated MyD88/IL1-RI interaction
Product does not compete with ATP.
Reversible: no
407272 Integrin αvβ3 Antagonist, P11 - Calbiochem The Integrin αvβ3 Antagonist, P11 controls the biological activity of Integrin αvβ3.  
K1513 Kendomycin from Streptomyces violaceoruber solid Potent endothelin receptor antagonist. Antiosteoporotic compound. Shows also remarkable antibacterial and cytotoxic activity. A putative cellular target for cytotoxicity has been identified: inhibition or altered regulation of the proteasome.
475878 (+)-MK 801 Maleate - CAS 77086-22-7 - Calbiochem A highly potent, selective, and non-competitive NMDA receptor antagonist that acts by binding to a site located within the NMDA-associated ion channel, thus preventing Ca2+ flux. Cell permeable: no
Primary Target
NMDA receptor
Reversible: no
480870 Neurotrophin Antagonist, Y1036 - Calbiochem The Neurotrophin Antagonist, Y1036 controls the biological activity of Neurotrophin. This small molecule/inhibitor is primarily used for Neuroscience applications.  
488230 Nogo-66 (1-40) Antagonist Peptide, Synthetic - Calbiochem Cell permeable: no
Primary Target
Nogo-66 receptor (NgR)
Product competes with ATP.
Reversible: no
511071 PAF Receptor Antagonist, ABT-491 - CAS 189689-94-9 - Calbiochem The PAF Receptor Antagonist, ABT-491, also referenced under CAS 189689-94-9, controls the biological activity of PAF Receptor. This small molecule/inhibitor is primarily used for Membrane applications.  
513020 PD 145065 - CAS 153049-49-1 - Calbiochem A highly potent but non-selective endothelin receptor antagonist [IC₅₀= 4 nM for the ETA receptor (rabbit renal artery vascular smooth muscle cells); IC₅₀ = 15 nM for the ETB receptor (rat cerebellum)]. Cell permeable: no
Primary Target
Endothelin receptor antagonist
Product does not compete with ATP.
Reversible: no
Target IC50: 4 nM against endothelin receptor (ETA receptor) in rabbit renal artery vascular smooth muscle cells; 15 nM for the ETB receptor (rat cerebellum)
PZ0141 PD-156707 ≥98% (HPLC) PD-156707 is a selective endothelin receptor (ETA) antagonist.
516567 PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem The PPARβ/δAntagonist II, PT-S58, also referenced under CAS 188591-46-0, controls the biological activity of PPARβ/δ. This small molecule/inhibitor is primarily used for Biochemicals applications.  
5370 L-Proline - CAS 147-85-3 - Calbiochem  
537075 (±)-Propranolol, Hydrochloride - CAS 3506-09-0 - Calbiochem A highly lipophilic agent that blocks both β₁ and β₂ adrenergic receptors with equal potency. A non-essential amino acid. Precursor of hydroxyproline in collagen. Cell permeable: no
Primary Target
β1 and β2 adrenergic receptors
Product does not compete with ATP.
Reversible: no
Target Ki: 17 nM for 5HT-1B receptors
553030 RAGE Antagonist, FPS-ZM1 - Calbiochem RAGE Antagonist, FPS-ZM1, is a blood-brain-barrier permeant blocker of RAGE V domain-mediated ligand binding (Ki = 25, 148, & 230 nM, respectively, against Aβ40, HMGB1 & S100B, binding to sRAGE). Cell permeable: yes
Primary Target
RAGE
Reversible: yes
Target Ki: 25, 148, and 230 nM, respectively, against A&beta
553031 RAGE Antagonist Peptide, RAP - Calbiochem The RAGE Antagonist Peptide, RAP controls the biological activity of RAGE. Primary Target
RAGE
Reversible: yes
559410 SB 290157 - CAS 1140525-25-2 - Calbiochem A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC₅₀ = 200 nM). Cell permeable: no
Primary Target
C3a receptor
Product does not compete with ATP.
Reversible: no
Target IC50: 200 nM against the anaphylatoxin C3a receptor; 7, 12.5, and 27.7 nM, in blocking C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR
PZ0203 Sitaxentan sodium salt ≥98% (HPLC) Sitaxentan (Sitaxsentan) is a potent and selective endothelin ET(A) receptor antagonist once used in the treatment of pulmonary arterial hypertension (PAH), but removed from the market because of hepatotoxicity. It is over 6000-fold selective for the the ETA receptor subtype with an IC50 of 1 nM for ETA versus an IC50 of 9800 nM for ETB.
Sitaxsentan prevents shunt mediated elevation of pulmonary vascular resistance (PVR). Sitaxsentan effectively inhibits basolateral Na+-taurocholate cotransporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and bile salt export pump (BSEP).
609315-M Thyroid Hormone Receptor Antagonist, 1-850 - CAS 251310-57-3 - Calbiochem The Thyroid Hormone Receptor Antagonist, 1-850, also referenced under CAS 251310-57-3, controls the biological activity of Thyroid Hormone Receptor. This small molecule/inhibitor is primarily used for Neuroscience applications. Primary Target
Thyroid Hormone Receptor
Target IC50: 1.5 µM as antagonist for thyroid hormone receptor (TR) in HeLa cells
648485-M TrpA1 Antagonist, HC-030031 - CAS 349085-38-7 - Calbiochem The TrpA1 Antagonist, HC-030031, also referenced under CAS 349085-38-7, controls the biological activity of TrpA1. This small molecule/inhibitor is primarily used for Neuroscience applications.  
616521 TRPV4 Antagonist II, HC-067047 - Calbiochem The TRPV4 Antagonist II, HC-067047 controls the biological activity of TRPV4.  
616520 TRPV4 Antagonist I, RN-1734 - CAS 946387-07-1 - Calbiochem The TRPV4 Antagonist I, RN-1734, also referenced under CAS 946387-07-1, controls the biological activity of TRPV4. This small molecule/inhibitor is primarily used for Biochemicals applications.  
SML1550 Zibotentan ≥98% (HPLC) Zibotentan has been found to inhibit cell proliferation, invasion and metastasis in cancer models. In clinical trials on patients with castration-resistant prostate cancer and bone metastasis, who were pain-free or had mild pain, zibotentan treatment resulted in better overall survival as compared to placebo.
Zibotentan is a potent and selective endothelin ET(A) receptor antagonist with an IC50 of 21 nM for the ETA receptor subtype and no binding observed even at 10,000 nM for ETB.