G-protein-coupled, nuclear and other ligand-binding receptors and their modulators.
Products may appear in more than one category. Counts refer to distinct catalog numbers within each category.
Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
Combine a keyword, research category and target to narrow the product list.
Loading catalog filters…
CAS 84371-65-3
Mifepristone (RU-486) is a potent steroidal antagonist exhibiting subnanomolar affinity for progesterone receptors (PR IC₅₀ = 0.2 nM) and nanomolar activity against glucocorticoid receptors (GR IC₅₀ = 2.6 nM). This dual-receptor modulator competitively blocks…
CAS 53714-56-0
Leuprolide is an agonist at pituitary GnRH receptors. Target: GnRH receptorLeuprorelin is a gonadotrophin-releasing hormone (GnRH) analogue used to treat a wide range of sex hormone-related disorders including advanced prostatic cancer, endometriosis and…
CAS 57773-63-4
Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferation
CAS 2212020-52-3
LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.
Eloralintide (LY 3841136) sodium is an AMYR agonist, which is promising for research of type 2 diabetes and obesity.
CAS 124750-99-8
Losartan (potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
CAS 849459-86-5
AC-263093 (AC263093) is a potent, functionally selective neuropeptide FF receptor type 2 (NPFFR2) agonist with pKi of 6.9; shows equal affinity for NPFFR1 and NPFFR2, and functionally inactivated NPFFR1; attenuates morphine tolerance in vivo.
CAS 190383-13-2
Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
CAS 1050656-06-8
MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to…
CAS 863704-91-0
PGN-9856 (PGN9856) is a novel potent, selective prostaglandin EP2 receptor agonist with pKi of > 8.3, shows higi selectivity over EP1 , EP3 , EP4 , DP, FP, IP and TP receptors; displays a potency (pEC50 >8.5) and a maximal response (increase in cAMP)…
CAS 854107-55-4
Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.
CAS 65928-58-7
Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis. Dienogest is an orally active synthetic progesterone (or progestin). It is available for use as an oral…
CAS 22978-25-2
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
CAS 153439-40-8
Fexofenadine is a third-generation antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria.
CAS 409351-28-6
VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
CAS 30123-17-2
Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.Tianeptine has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant,…
CAS 357-08-4
Naloxone is an opioid inverse agonist drug used to counter the effects of opiate overdose.
CAS 361187-13-5
NCGC00161856 is identified as the first small-molecule ligand and inverse agonist of the thyroid-stimulating hormone receptor (TSHR). It inhibits basal cAMP production in HEK-EM 293 cells that stably express TSHRs, with a half-maximal inhibitory concentration…
CAS 2151041-09-5
STD-101-D1 is a novel brain permeable, G protein-biased beta-1 adrenergic receptor (ADRB1) partial agonist with EC50 of 16.9 nM; engages very little beta-arrestin recruitment compared to the unbiased agonist isoproterenol; also inhibits the acute peripheral…
CAS 1119831-25-2
S6821 (S 6821) is a potent and selective antagonist of the bitter taste receptor TAS2R8, exhibiting an IC50 value of 21 nM. It demonstrates high selectivity across a panel of 16 TAS2Rs, effectively reduces the bitterness of coffee, and shows an excellent…
GHSR1a agonist with binding IC50 of 1.3 uM.N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible…
CAS 2490544-50-6
TG8-260 is a second-generation, potent, selective EP2 antagonist with Schild KB of 13.2 nM.TG8-260 displays 500-fold selectivity to EP2 against other prostanoid receptors.TG8-260 has a plasma half-life of 2.14 h (PO) and excellent oral bioavailability…
CAS 2924984-09-6
ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces…
CAS 62-97-5
Diphemanil methylsulfate is a quaternary ammonium anticholinergic. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat.
CAS 1263409-34-2
AM 432 is potent, selective, orally active prostaglandin D2 receptor (DP2/CRTH2) antagonist with binding IC50 of 6 nM for hDP2; shows no cross-reactivity against the TP or IP receptors, COX-1 or COX-2 and minimal activity at DP1 receptor; shows excellent…
CAS 1613028-81-1
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
CAS 124750-92-1
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks…
CAS 152918-18-8
Piclidenoson (IB-MECA) is an agonist of the adenosine A3 receptor with EC50 values of 0.11 μM.
CAS 1334237-71-6
Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis…
CAS 129311-55-3
Ganirelix acetate is an antagonist of GnRH that competitively antagonizes the gonadotropic GnRH receptor, thereby mutating the pathway and causing rapid and reversible inhibition of gonadotropin (luteinizing hormone LH and follicle stimulating hormone FSH)…
CAS 440122-66-7
WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.
CAS 175140-00-8
CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.
CAS 201038-74-6
SB269970 is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.
CAS 945128-26-7
CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.
CAS 158681-13-1
Rimonabant hydrochloride is a cannabinoid receptor (CB) antagonist which binds selectively to CB1 with a Ki of 2 nM.
CAS 19356-17-3
Calcifediol is a major circulating metabolite of vitamin D3, acting as a competitive inhibitor with an apparent Ki of 3.9 μM, suppresses PTH secretion and mRNA (ED50=2 nM).
CAS 107008-28-6
RU 24969 hemisuccinate is a potent SR-1A/SR-1B and moderate SR-2C agonist that may also release serotonin.
CAS 115103-85-0
MK-571 sodium salt (L-660711) is a selective, orally active antagonist of leukotriene D4 receptor. It is also an inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1).
CAS 37025-55-1
Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
CAS 596-51-0
Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive antagonist used as an antispasmodic.
CAS 138614-30-9
Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively[1][2][3].
CAS 104344-23-2
Bisoprolol, on beta 1-adrenoceptor pBisoprolol is a selective type β1 adrenergic receptor blocker.Approved: July 31, 1992Bisoprolol, on beta 1-adrenoceptor peptide induced autoimmune myocardial damage. In the animal model of autoimmune cardiomyopathy induced…
