LY83583 is a cell-permeable and competitive inhibitor of soluble guanylate cyclase (sGC) with an IC50 value of 2 µM[1].
Amelubant (BIIL 284) is a potent, oral and long acting LTB4 receptor antagonist, negligibly binds to LTB4 receptor, with Kis of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity[1].
Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability[1].
Melatonin D5 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4].
DL-Norepinephrine-d3 (hydrochloride) is the deuterium labeled DL-Norepinephrine hydrochloride[1]. DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension[2].
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM[1].
CRF,bovine is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM.
Protokylol (Caytine; JB-251) is a beta-adrenergic receptor agonist and TRPV1 agonist. Protokylol is used as a bronchodilator[1].
Doxylamine is a first generation antihistamine; can be used by itself as a short-term sedative and in combination with other drugs to provide night-time allergy and cold relief.
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis[1][2].
BMS-986188 is a selective positive allosteric modulator of δ-opioid receptor with an EC50 of 0.05 μM[1].
Eucatropine is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC50 value of 0.583 μM. Eucatropine is an anticholinergic agent[1].
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research[1].
N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect[1]-[5].
SOS1-IN-4 is a potent SOS1 inhibitor with an IC50 of 56 nM for KRAS-C12C/SOS1 interaction (WO2021228028 A1, example 65)[1].
Trihexyphenidyl is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research[1][2].
Propantheline is an orally active mAChR antagonist. Propantheline can be used in the research of smooth muscle dysfunction, excessive sweating, cramps or spasms of the stomach, intestines or bladder, and involuntary urination[1][2][3].
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
LY 293284 is a potent and selective 5-HT1A receptor agonist. LY 293284 results in a significant drop in core temperature and consumes more food in cholestasis rat induced by bile duct resection[1][2].
CYM-5482 is a potent and selective agonist Sphingosine 1-phosphate receptor 2 (S1PR2) with an IC50 and EC50 of 1.0 and 1.03 μM. CYM-5482 has the potential for the research of cancer diseases[1].
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor. Sequence: Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Lys-Ala-Phe.
Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
15-keto-Prostaglandin F2α (15-keto-PGF2α) is a metabolite of Prostaglandin F2α. Prostaglandin F2α. Prostaglandin F2α is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist and plays a key role in the onset and progression of labour[1].
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors[1].
Trazodone (AF-1161 free base) is a serotonin receptor antagonist and reuptake inhibitor. Trazodone can be used for the research of major depressive disorder. Trazodone also has potential for sleep disorder research[1].
NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).IC50 value: 16/11 nM(Binding/Functional IC50) [1]Target: EBI2/GPR183 antagonistNIBR189 is a potent and selective EBI2 antagonist with improved pharmacokinetic properties which will help to probe the physiological function of EBI2 in health and disease.