H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, with IC50s of 94, 752, and 463 nM respectively.

Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R.

K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.

CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity.

RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).

Novokinin TFA is a peptide agonist of the angiotensin AT2 receptor.

Angiotensin I/II (1-6) TFA contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. The precursor angiotensinogen is cleaved by renin to form angiotensin I. Angiotensin I ishydrolyzed by angiotensin-converting enzyme (ACE) to form the biologically active angiotensin II. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.

Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium.

FFN270 hydrochloride, a fluorescent tracer of norepinephrine, is a fluorescent substrate of the norepinephrine and vesicular monoamine transporters. FFN270 hydrochloride exhibits two resolved absorption/excitation maxima depending on solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm) and can function as ratiometric fluorescent pH-sensors.

O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.

Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor.

Ro 363 hydrochloride is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.

NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.

SGS518 oxalate is a selective 5-HT6R antagonist. SGS518 oxalate can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses[1]

Protirelin (Thyrotropin-releasing-hormone, TRH, Thyroliberin) acetate is a highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions.

L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic respon

Butaprost is a selective prostaglandin E receptor (EP2) agonist with a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost effectively mitigates renal fibrogenesis.

6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.

JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of [125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly p

[D-Arg25]-Neuropeptide Y (human) ([D-Arg25] NPY) is a Y1 receptor selective agonist. Neuropeptide Y (human) is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity.

2-Oleoylglycerol is a dietary naturally occurring lipid. 2-Oleoylglycerol is a GPR119 agonist, with an EC50 of 2.5 μM for human GPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol stimulates glucagon-like peptide-1 (GLP-1) secretion in vivo.

PD 168568 dihydrochloride is an orally active and selective D4 dopamine receptor antagonist, with a Ki of 8.8 nM.

PNU-177864 hydrochloride is a potent, selective and orally active dopamine D3 receptor antagonist. PNU-177864 hydrochloride is structurally consistent with a cationic amphiphilic drug (CAD) and induces phospholipidosis in vivo. PNU-177864 hydrochloride an

SB-203186 hydrochloride is a potent and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.

Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.

Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.

Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties.

Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.