subtype

BIBO3304 TFA is an effective, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist (IC50:0.38 and 0.72 nM for the human and the rat Y1 receptor).

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).

Difamilast is an inhibitor of phosphodiesterase IV.

Radioprotectin-1 is a selective agonist of LPA2 with EC50 of 25 nM for murine LPA2 GPCR and exerts radioprotective and radiomitigative action.

Camonagrel is a compound with inhibitory effects on Prostaglandin E2 (PGE2).

HEMADO is a potent and selective agonist of the adenosine A3 receptor [Ki: 1.1 nM at the human A3 subtype].

Afloqualone (HQ-495) is a quinazolinone family GABAergic drug that acts as an agonist of the β subtype of the GABAa receptor, exhibiting sedative and muscle-relaxant effects.

ETHYL 2-AMINO-4-METHYL-5-PHENYLTHIOPHENE-3-CARBOXYLATE targets the prostaglandin E2 receptor EP2 subtype (human)

Insulin efsitora alfa (LY-3209590) is a selective insulin receptor (IR) agonist and fusion protein that combines a novel single-chain insulin variant with the structural domain of human IgG Fc for the study of type 2 diabetes.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

(R)-Terazosin is an active R-enantiomer of Terazosin and a potent antagonist of α1-adrenoceptor [(α1a, α1b, and α1d-adrenoceptor] with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively).

Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

GW3965 hydrochloride (GW3965 HCl) belongs to synthetic small molecules and is a liver X receptor (LXR) agonist (hLXRα EC50 = 190 nM; hLXRβ EC50 = 30 nM) with subtype selectivity, cell permeability, and oral activity. This compound is used in research related to metabolism, inflammation, and neuropathic pain.

Urotensin I acetate (83930-33-0 Free base) is a CRF-like neuropeptide (natural product), a CRF receptor agonist (EC50 as low as 3.5 pM for hCRF1, Ki=0.4 nM), with high affinity and receptor subtype selectivity, used for CRF receptor functional research.

Rivanicline 2HCl is a selective neuronal nicotinic receptor inhibitor with a high affinity for the α4β2 subtype.

UB 165 fumarate is an agonist of the nAChR, a partial agonist of the α4β2 subtype, and a full agonist of the α3β2 subtype, with a Ki value of 0.27 nM for binding to [3H]-nicotine measured in rat brain.

SIB 1553A is an orally available and selective agonist of nicotinic acetylcholine receptors (nAChRs), which are subtype-selective ligands for nicotinic acetylcholine receptors.SIB-1553A is a cognitive enhancer that may be used in the study of neurodegenerative-related diseases such as Alzheimer's disease.

BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth and demonstrates inhibitory activity against certain subtypes of influenza viruses. BMY-27709 acts early in H1 and H2 virus infections by inhibiting hemagglutinin proteins but has no effect on H3 subtype viruses and influenza B/Lee/40 viruses.

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist used to study diseases of the biblical system and metabolism-related diseases.

Cyclazosin HCl is a subtype-selective α-adrenergic receptor antagonist that competitively antagonizes norepinephrine-induced α(1B)-adrenergic receptor contraction and can be used to study non-arteritic ischemic optic neuropathy and other neurological diseases.