Agonists

Endothelin

The endothelins are the strongest vasoconstrictors known, acting to maintain vascular tone. In addition, they have multiple effects on disparate systems: such as sodium balance, heart rhythm, neural development, and vascular endothelial proliferation. Three 21-residue endothelin peptides with two disulfide bridges are encoded by three genes and differ somewhat in their physiological roles.1 Thus far only two receptors, ETA and ETB, have been described. These receptors are linked to a Gq protein. We offer very pure human endothelins 1,2, and 3 as receptor agonists. Two linear peptides that lack disulfide bridges, BQ-3020 and (Ala 1,3,11,15)-Endothelin 1, are specific agonists for the ETB receptor.

Endothelins have been highly conserved in evolution. Venom from the Atractaspis engaddensis viper contains three isototoxins that are highly analogous to endothelins and bind to cardiac endothelin receptors. A bite from this snake can disrupt heart rhythm and constrict coronary vessels enough to cause death within minutes. One venom isoform, sarafotoxin S6b is an ETA agonist, while isoform sarafotoxin S6c is an ETB agonist.

1. Inoue, A., et al. Proc. Natl. Acad. Sci. U. S. A. 86, 2863-2867, (1989)

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119134 Adenosine 5ʹ-O-(2-Thiodiphosphate), Trilithium Salt - CAS 73536-95-5 - Calbiochem A P₂-purinergic receptor agonist that acts as a potent insulin secretagogue. Cell permeable: no
Primary Target
A P2-purinergic receptor agonist
Product does not compete with ATP.
Reversible: no
1191 Adenosine 5ʹ-Triphosphate, Disodium Salt - CAS 987-65-5 - Calbiochem  
182690 AhR Agonist V, VAF347 - Calbiochem The AhR Agonist V, VAF347 controls the biological activity of AhR. This small molecule/inhibitor is primarily used for Biochemicals applications.  
149101-M 1-Aminocyclopropane-1-carboxylic Acid - CAS 22059-21-8 - Calbiochem An agonist for the glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor complex. Primary Target
Glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor complex
Target IC50: 38 nM in blocking 3H-glycine binding to rat forebrain membrane; 131 µM in blocking NMDA-induced release of arachidonic acid; 131 µM in cerebellar granule cells
165300 L-(+)-2-Amino-4-phosphonobutyric Acid - CAS 23052-81-5 - Calbiochem  
SCP0138 BQ-3020 BQ-3020, a linear endothelin analog, is a selective ETB endothelin receptor agonist.
212385-M Carbachol - CAS 51-83-2 - Calbiochem An unsubstituted carbamoyl ester that acts as an agonist for nicotinic and muscarinic acetylcholine receptors. Primary Target
Agonist for nicotinic and muscarinic acetylcholine receptors
239823 CXCR3 Agonist, PS372424 - Calbiochem The CXCR3 Agonist, PS372424 controls the biological activity of CXCR3. This small molecule/inhibitor is primarily used for Cell Signaling applications.  
239824 CXCR7 Agonist, VUF11207 - Calbiochem The CXCR7 Agonist, VUF11207 controls the biological activity of CXCR7. This small molecule/inhibitor is primarily used for Biochemicals applications. Cell permeable: yes
Primary Target
CXCR7
Reversible: yes
128136 7α, 25-dihydroxycholesterol - Calbiochem  
E7764 Endothelin 1 ≥97% (HPLC), powder Endothelin-1 (ET-1) is a vasoconstrictor, which is increased in plasma and explants of patients with uterine leiomyomas. Thus, uterine fibroids are linked to increased ET-1 levels and hypertension, which is worsened by hypoxic condtions. ET-1 RNAi and Endostar are capable of preventing the progression and invasiveness of PC-3 (prostate cancer) cells. The plasma levels of this peptide are increased in patients with atrial septal defect (ASD), and these levels might help in diagnosis of closure defects. The plasma level of ET-1 is also higher in patients with end-stage renal disease (ESRD), and this is linked to gradual worsening of pulmonary function tests.
Potent agonist for ETA and ETB endothelin receptors. Induces the production of hypoxia-inducible factor 1α, and, thus, the production of VEGF.
E6877 [Ala1,3,11,15]-Endothelin 1 Selective agonist for ETB endothelin receptors.
E9012 Endothelin 2 human ≥97% (HPLC), powder Endothelin-2 (ET-2) has a regulatory role in multiple cancer types, such as breast and clear cell renal cell carcinoma (ccRCC). It is overexpressed during early stages of non-metastasized ccRCC, and is thought have a role in the progression of the same. It is a hypoxia-related factor, and might have protective action against cell death in neuronal diseases. It acts as a ligand for ET-A and ET-B receptors, which results in vasoconstriction. A985 polymorphism in this gene is thought play a protective role in cardiovascular diseases, but it acts as a susceptibility factor in atrial fibrillation in hypertrophic cardiomyopathy patients. In neural retina, it suppresses angiogenesis, and facilitates the tip cell state in endothelial cells.
E9137 Endothelin 3 human, rat ≥97% (HPLC), powder Endothelin 3 (ET3) is a vasoconstrictor that acts in a paracrine and autocrine manner, and in intestinal lamina propria causes the degranulation of mast cells. It results in the release of ions from intestinal epithelial cells. In acute and chronic intestinal inflammation, it is overexpressed. It is also up-regulated in colon carcinoma, where it supports cell proliferation and survival. It might be involved in colon homeostasis, and is essential for the survival and proliferation of goblet cells. In mice, it is essential for the development of pigment cells derived from neural crest (NC). Its expression is de-regulated in metastatic melanoma.
Potent vasoconstrictor from vascular endothelial cells; preferred agonist for ETB endothelin receptors. Induces the production of VEGF.
324900 L-(–)-Epinephrine-(+)-bitartrate - CAS 51-42-3 - Calbiochem α,β-Adrenergic receptor agonist. Cell permeable: no
Primary Target
α,β-Adrenergic receptor agonist
Product does not compete with ATP.
Reversible: no
346007 Glucagon-Like Peptide 1 Receptor Agonist II - Calbiochem  
371709 GPR109b Agonist - CAS 306935-41-1 - Calbiochem The GPR109b Agonist, also referenced under CAS 306935-41-1, controls the biological activity of GPR109b. This small molecule/inhibitor is primarily used for Activators/Inducers applications.  
371706 GPR40 Agonist - CAS 885101-89-3 - Calbiochem The GPR40 Agonist, also referenced under CAS 885101-89-3, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Cell Signaling applications.  
370625 Guanabenz Acetate - CAS 23256-50-0 - Calbiochem A cell-permeable α2-adrenoceptor agonist that lowers protein misfolding in stressed cells and acts as a proteostatis regulator.  
566661 InSolution Smoothened Agonist, SAG - Calbiochem InSolution Smoothened Agonist, SAG, is a 10 mM (500 µg/86 µl) solution of Smoothened Agonist, SAG (Cat. No. 566660) in H₂O.  
420355 Isoproterenol, Hydrochloride - CAS 51-30-9 - Calbiochem Phenethylamine derivative. Cell permeable: no
Primary Target
β-adrenergic agonist
Product does not compete with ATP.
Reversible: no
420318 Kainic Acid - CAS 487-79-6 - Calbiochem An excitatory amino acid receptor agonist selective for the kainate receptor subtype (Ki = 21 nM for ³H-kainate binding in rat striatum). Cell permeable: no
Primary Target
Kainate receptor subtype
Product does not compete with ATP.
Reversible: no
Target Ki: 21 nM for 3H-kainate binding in rat striatum
445888 Metastin (45-54) - Calbiochem A decapeptide with C-terminally amidated LRF-motif that acts as a potent and selective agonist of AXOR12 and hOT7T175 (a novel human G-protein-coupled receptors). Cell permeable: no
Primary Target
AXOR12 and hOT7T175
Product does not compete with ATP.
Reversible: no
Target Ki: 42 pM for AXOR12 and hOT7T175
481975 (--)-Nicotine, Ditartrate - CAS 65-31-6 - Calbiochem Potent agonist of the nicotinic acetylcholine receptor. Cell permeable: no
Primary Target
Nicotinic acetylcholine receptor
Product does not compete with ATP.
Reversible: no
489350 L-(–)-Norepinephrine-(+)-bitartrate - CAS 69815-49-2 - Calbiochem α,β-Adrenergic agonist. Cell permeable: no
Primary Target
α,β-Adrenergic agonist
Product does not compete with ATP.
Reversible: no
539109 PAR-2 Agonist I - Calbiochem The PAR-2 Agonist I controls the biological activity of PAR-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications. Cell permeable: no
EC50 = 253 nM as PAR-2-specific agonist using HCT-15 cells
Primary Target
PAR-2
Product does not compete with ATP.
Reversible: no
528201 PNU-120596 - CAS 501925-31-1 - Calbiochem A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors  
554716 REV-ERBα Agonist, GSK4112 - Calbiochem The REV-ERBα Agonist, GSK4112 controls the biological activity of REV-ERBα. This small molecule/inhibitor is primarily used for Biochemicals applications.  
554726 REV-ERB Agonist II, SR9009 - Calbiochem The REV-ERB Agonist II, SR9009 controls the biological activity of REV-ERB. This small molecule/inhibitor is primarily used for Biochemicals applications. Cell permeable: yes
Primary Target
REV-ERB-α/&beta
Reversible: yes
557352 RORα/γ Agonist, SR1078 - Calbiochem The RORα/γ Agonist, SR1078 controls the biological activity of RORα/γ. This small molecule/inhibitor is primarily used for Biochemicals applications. Cell permeable: yes
Primary Target
RORα/γ
Reversible: yes
S1522 Sarafotoxin S6a1 ≥97% (HPLC)  
S6545 Sarafotoxin S6c ≥97% (HPLC) Sarafotoxin S6c is an endothelin ETB agonist. It is a peptide isotoxin with strong vasoconstrictor activity, obtained from the Middle Eastern snake, Atractaspis engaddensi. The toxin is composed of 21 amino acids.
566660 Smoothened Agonist, SAG - CAS 364590-63-6 - Calbiochem A cell-permeable Smoothened Agonist, SAG, CAS 364590-63-6, modulates the coupling of Smo with its downstream effector by interacting with the Smo heptahelical domain (KD = 59 nM).  
5677 Spermine, Tetrahydrochloride - CAS 306-67-2 - Calbiochem Primary Target
phospholipase C α
Secondary Target
nNOS
605208 Thrombin Receptor Agonist - CAS 137339-65-2 - Calbiochem The Thrombin Receptor Agonist, also referenced under CAS 137339-65-2, controls the biological activity of Thrombin Receptor. This small molecule/inhibitor is primarily used for Activators/Inducers applications. Cell permeable: no
Primary Target
Thrombin Receptor
Product does not compete with ATP.
Reversible: no
648493-M TRPML Agonist, ML-SA1 - CAS 332382-54-4 - Calbiochem The TRPML Agonist, ML-SA1 controls the biological activity of TRPML. This small molecule/inhibitor is primarily used for Biochemicals applications. Primary Target
TRPML1,2,3
681665 Wnt Agonist - CAS 853220-52-7 - Calbiochem The Wnt Agonist, also referenced under CAS 853220-52-7, controls the biological activity of Wnt. This small molecule/inhibitor is primarily used for Cancer applications. Cell permeable: yes
EC50 = 700 nM inducing β-catenin and TCF (T-cell fate)-dependent transcriptional activity in HEK-293T cells
Primary Target
Selective activator of Wnt signaling
Product does not compete with ATP.
Reversible: no
681667 Wnt Agonist II, SKL2001 - Calbiochem The Wnt Agonist II, SKL2001 controls the biological activity of Wnt. This small molecule/inhibitor is primarily used for Biochemicals applications.  
681664 Wnt Agonist I in DMSO - CAS 853220-52-7 - Calbiochem The Wnt Agonist I in DMSO, also referenced under CAS 853220-52-7, controls the biological activity of Wnt. This small molecule/inhibitor is primarily used for Cancer applications. Cell permeable: yes
Reversible: yes