GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR-196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice.
YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
Guanabenz Acetate is an alpha-2 selective adrenergic agonist used as an antihypertensive agent.Target: alpha-2 Adrenergic ReceptorGuanabenz is an alpha agonist of the alpha-2 type that is used as an antihypertensive drug. It is used to treat high blood pressure (hypertension) [1, 2].
IRL 1038 is an endothelin B receptor selective antagonist with a Ki of 6-11 nM[1].
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant mGluR4 positive allosteric modulator (PAM) with an EC50 of 79 nM[1]. Antiparkinsonian effect[1].
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr)[1].
Pirnabine is a cannabinoid receptor ligand. Pirnabine can be used for the research of glaucoma[1].
GSK2041706A (GSK706) is a potent G protein-coupled receptor 119 (GPR119) agonist. GSK2041706A can be used for the research of type 2 diabetes[1].
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells.
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research[1].
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues[1].
Fenoldopam-d4 (SKF-82526-d4) mesylate is the deuterium labeled Fenoldopam mesylate. Fenoldopam (SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist[1][2].
(S)-4CPG ((S)-4-Carboxyphenylglycine) is a potent mGluR2 agonist. (S)-4CPG reduces hyperalgesia and allodynia associated with sciatic nerve contraction injury in rats. (S)-4CPG can be used in research on neurological diseases[1][2].
Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.Target: Type-1 angiotensin II receptorCandesartan is generally well tolerated and significantly reduced cardiovascular deaths and hospital admissions for heart failure. Ejection fraction or treatment at baseline did not alter these effects [1]. In rats, TCV-116 inhibited the pressor responses to Ang I, Ang II, and Ang III without an effect on the bradykinin (BK)-induced depressor response. In SHR, the antihypertensive effect of TCV-116 (10 mg/kg) was larger than the maximum antihypertensive effect of enalapril and was not intensified by combination with enalapril. TCV-116 is more effective than enalapril in reducing blood pressure in SHR and 1K, 1C-HR, and that the BK- and/or prostaglandin-potentiating effect of enalapril contributes little to its antihypertensive mechanism in SHR [2].
Glucagon-Like Peptide (GLP) I (7-36), amide, human is a physiological incretin hormone that stimulates insulin secretion.
Droperidol is a Dopamine-2 Receptor Antagonist. Target: D2DRDroperidol is a butyrophenone, with anti-emetic, sedative and anti-anxiety properties.
CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration[1].
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis[1][2][3].
GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM[1]. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo[2].
5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.
Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.Target: Angiotensin ReceptorIrbesartan treatment markedly induces the expression of the adipogenic marker gene adipose protein 2 (aP2) in 3T3-L1 cells in a concentration-dependent manner with EC50 of 3.5 μM and 3.3-fold induction at the concentration of 10 μM. Irbesartan (10 μM) markedly induces transcriptional activity of the peroxisome proliferator–activated receptor-γ (PPARγ) by 3.4-fold independent of its AT1 receptor blocking action. Pretreatment with Irbesartan (~10 μM) decreases angiotensin II-induced apoptosis in rat vascular smooth muscle cells by blocking angiotensin II internalization in a concentrationdependent manner. Oral administration of Irbesartan (1 mg/kg) reduces angiotensin II (AII)-induced hypertension, equipotent with losartan in conscious normotensive rats, markedly more active than losartan (10 mg/kg) in normotensive cynomolgus monkeys. Administration of Irbesartan (7 mg/kg/day) significantly prevents skeletal muscle apoptosis and muscle atrophy in rats with monocrotaline-induced congestive heart failure (CHF), which is involved with the decrease of TNFα level and attributed to AT1 receptor blocking.
RTIOXA-43 is a orexin receptor agonist with EC50s of 24 nM and 24 nM for OX2 and OX1 receptors, respectively[1].
Naratriptan hydrochloride is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.Target: 5-HT1 ReceptorNaratriptan is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. Naratriptan is available in 2.5 mg tablets. It is a selective 5-HT1 receptor subtype agonist. Naratriptan is used for the treatment of the acute migraine attacks and the symptoms of migraine, including severe, throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound or light.The causes of migraine are not clearly understood; however, the efficacy of naratriptans and other triptans is believed to be due to their activity as 5HT (serotonin) agonists.A meta-analysis of 53 clinical trials has shown that all triptans are effective for treating migraine at marketed doses and that naratriptan, although less effective than sumatriptan and rizatriptan was more effective than placebo in reducing migraine symptoms at two hours and efficacy was demonstrated in almost two thirds of subjects after four hours of treatment.
Doxepin D3 Hydrochloride is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant used as a sedative. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect[1][2].
Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity[1].