et receptor antagonist 1 — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T79573	ET receptor antagonist 1		Estrogen Receptor/ERR
	ET Receptor Antagonist 1 (compound 16h), with an IC50 value of 0.18 nM, is an orally active agent that can be utilized for pulmonary arterial hypertension (PAH) research. It has demonstrated efficacy in mitigating monocr...		Estrogen Receptor/ERR
T10595	BQ-788	BQ788	Endothelin Receptor
	BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion press...		Endothelin Receptor
T3194	Ro 46-2005		Endothelin Receptor
	Ro 46-2005 is a synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor, IC50: 220 nM).		Endothelin Receptor
T36008	Nebentan potassium
	Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned ...
T36949	Niaprazine		5-HT Receptor , Adrenergic Receptor , Histamine Receptor
	Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2]. Niaprazine exhibits a low aff...		5-HT Receptor , Adrenergic Receptor , Histamine Receptor
T6264	Bosentan	Actelion,Ro 47-0203,Benzenesulfonamide	Endothelin Receptor
	Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks th...		Endothelin Receptor
T37816	SB 243213
	SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range o...
T38192	Unifiram		Others
	Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the ra...		Others
T35623	ACT-373898
	ACT-373898 is a metabolite of the endothelin (ET) receptor type A (ETA) and ETBdual antagonist macitentan .1 1.Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan...
T79574	ET receptor antagonist 2		Estrogen Receptor/ERR
	ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced...		Estrogen Receptor/ERR
T34762	T-0201	T 0201,TA0201,TA-0201,TA 0201
	T-0201 (TA 0201) is a highly potent, long-acting, orally active, and selective ETA receptor antagonist. T-0201 also inhibited ET-1-induced pulmonary artery contraction in isolated rabbits.
T79575	ET receptor antagonist 3		Estrogen Receptor/ERR
	"ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH) research. This compound demonstrates efficacy in mitigating ...		Estrogen Receptor/ERR
T27647	J-104132	L753037,L 753037,J104132,J 104132,L-753037
	J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inosito...
T36374	Naloxegol (NKTR-118)
	Naloxegol (NKTR-118; AZ-13337019) is an opioid-receptor antagonist[1]. [1]. Yoon SC, et al. Naloxegol in opioid-induced constipation: a new paradigm in the treatment of a common problem. Patient Prefer Adherence. 2017 Ju...
T76633	(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
	(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin, a potent vasopressin V1 receptor (VP V1R) antagonist, significantly lowers mean arterial pressure (MAP) in rats [1].
T38169	LY 341495 disodium salt
	Highly potent and selective group II metabotropic glutamate receptor antagonist. Disodium salt of LY 341495 Fitzjohn et al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mG...
T64084	Clazosentan
	Clazosentan (Ro 61-1790) is a selective antagonist of the endothelin A receptor (ETAreceptor) and exhibits an inhibitory effect on ET-1-mediated vasoconstriction.Clazosentan prevents cerebral vasospasm and vasospasm-asso...
T37014	Inupadenant
	Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity[1]. [1]. Laurence Buisseret, et al. Phase 1 trial of the adenosine...
T38228	R 121919 hydrochloride
	High affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable. Chen and Grigoriadis (...
T38323	A-943931 (hydrochloride hydrate)
	A-943931 is a histamine H4receptor antagonist (Ki= 3.8 nM).1In vivo, A-943931 inhibits scratching induced by clobenpropit in mice (ED50= 26 μmoles/kg, i.p.). 1.Milicic, I., Witte, D.G., Miller, T.L., et al.Identification...