GPCRs & Receptor Biology

PRE-084 hydrochloride

CAS 138847-85-5

PRE-084 hydrochloride is a high affinity, selective σ1 agonist (Ki values are 2.2 and 13091 nM for σ1 and σ2 receptors respectively).

MRS-1706

CAS 264622-53-9

MRS-1706 is a potent and selective A(2B) adenosine receptor antagonist with a Ki value of 1.39 nM.

Ostarine(MK-2286)

CAS 841205-47-8

Ostarine(MK-2866; GTX-024) is a modulator of human androgen receptor.IC50 value:Target: androgen receptorOstarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases…

Enzalutamide (MDV3100)

CAS 915087-33-1

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

ARV-110

CAS 2222112-77-6

ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer.

T0070907

CAS 313516-66-4

T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.

DIM-C-pPhOH(CDIM8)

CAS 151358-47-3

DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O…

GLPG2938

CAS 2130996-00-6

GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis[1].

Bremelanotide acetate

CAS 1607799-13-2

Bremelanotide Acetate is a melanocortin agonist.IC50 value:Target: melanocortinin vivo: Bremelanotide is a novel drug candidate for the treatment of male and female sexual dysfunction. Bremelanotide has shown promise in effectively treating erectile…

Naltrexone

CAS 16590-41-3

A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively; also inhibits IL-6 and TNFα production in human immune cell subsets following stimulation with ligands for…

Decoglurant

CAS 911115-16-7

Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant[1].

SB-334867 HCl

CAS 249889-64-3

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. IC50 value: 7.2 (pKb) Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses…

Solabegron

CAS 252920-94-8

Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM[1]. Solabegron (GW 427353) is being developed for the treatment of…

EMPA

CAS 680590-49-2

EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively[1].

PD-168077 maleate

CAS 630117-19-0

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

Dinoprost

CAS 551-11-1

Dinoprost(Prostaglandin F2α) is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.

ML221

CAS 877636-42-5

ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.

Alexamorelin

CAS 196808-85-2

Alexamorelin is a new synthetic heptapeptide which inhibits GHS binding in vitro.

Idalopirdine Hydrochloride

CAS 467458-02-2

Idalopirdine, also known as Lu AE58054 or Iladopirdine, is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.…

Histrelin acetate

CAS 220810-26-4

Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor).

ASC-J9

CAS 917813-54-8

For the detailed information about the solubility of ASC-J9 in water, the solubility of ASC-J9 in DMSO, the solubility of ASC-J9 in PBS buffer, the animal experiment（test） of ASC-J9, the in vivo,in vitro and clinical trial test of ASC-J9, the cell…

SR3335

CAS 293753-05-6

SR3335 (ML-176) is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays. Furthermore, SR3335 suppresses the expression of endogenous RORα target genes…

Balovaptan

CAS 1228088-30-9

Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.

ADL5859 HCl

CAS 850173-95-4

ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. IC50 value: 0.8 nM(Ki)Target: δ-opioid receptorADL-5859 (ADL5859) is an δ-opioid receptor agonist (Ki=0.84…

DALDA

CAS 118476-85-0

DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) is a potent μ-opioid peptide agonist, affecting various patterns of locomotor activities.

E4CPG

CAS 170846-89-6

E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .

ML401 (CID73169083)

CAS 1597489-14-9

ML401, a potent chemical probe, selectively antagonizes EBI2 (also known as GPR183) with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity[1].

Giredestrant

CAS 1953133-47-5

Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain.…

Pramipexole 2HCL monohydrate

CAS 191217-81-9

Pramipexole dihydrochloride hydrate is a selective dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research…

Cortagine

Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.

Semaglutide (sodium salt)

CAS 910463-68-2

Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.

Octreotide acetate (SMS 201-995 (acetate))

CAS 79517-01-4

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

Cetirizine 2HCl

CAS 83881-52-1

Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.Cetirizine crosses the blood-brain barrier…

Mirabegron

CAS 223673-61-8

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

TAK-875(Fasiglifam)

CAS 1000413-72-8

Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

PD-123319 free base

CAS 130663-39-7

PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

Apararenone

CAS 945966-46-1

Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.

ML382

CAS 1646499-97-9

ML382 is a potent, selective, positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1) with EC50 of 190 nM in cell based Ca2+ imaging assay; displays >100-fold selectivity versus MrgX2; enhances the ability of BAM8-22 to inhibit…

BUN79398

CAS 2377379-39-8

BUN79398(MRGPRX1 agonist 1) is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect[1].

ZB716(Fulvestrant-3 Boronic Acid)

CAS 1853279-29-4

ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells.

Cenicriviroc

CAS 497223-25-3

Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.

Calcitonin salmon

CAS 47931-85-1

Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption. Sequence:…

Tirzepatide (LY3298176)

CAS 2023788-19-2

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

Plerixafor (AMD3100)

CAS 110078-46-1

Plerixafor is a selective CXCR4 antagonist with an IC50 of 44 nM.

Mesdopetam hemitartrate

CAS 2562346-14-7

Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in…

IMTPPE

CAS 851688-13-6

IMTPPE (SID 3712502) is a novel small molecule capable of inhibiting androgen receptor (AR) transcriptional activity (IC50=1 uM) and protein level in C4-2 prostate cancer cells; IMTPPE inhibited proliferation of AR-positive, but not AR-negative, prostate…

AR 231453

CAS 733750-99-7

AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.

ZM241385

CAS 139180-30-6

ZM 241385 is a selective and high affinity A2A adenosine receptor antagonist.