GPCRs & Receptor Biology

AM966

CAS 1228690-19-4

AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).

SR-12813（GW 485801）

CAS 126411-39-0

SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.

MDK-5220(Orexin-2 receptor agonist)

CAS 1796565-52-0

Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.IC50 value: 23 nM (EC50)Target: Orexin 2 ReceptorOrexin 2 Receptor Agonist shows not only potentactivity but also high selectivity for OX2R…

BIBS39

CAS 133085-33-3

BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.

APD597(JNJ-38431055)

CAS 897732-93-3

APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.

Tazarotenic acid (AGN 190299)

CAS 118292-41-4

Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma[1][2][3].

Olanzapine

CAS 132539-06-1

Olanzapine(LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.IC50 Value:Target: 5-HT ReceptorOlanzapine is a thienobenzodiazepine that blocks especially the serontonin (5-hydroxytryptamine [5-HT]) 5-HT2A and the dopamine D2…

RU58841

CAS 154992-24-2

RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 (PSK-3841) has a dramatic effect on hair regrowth.

Macitentan (Actelion-1,ACT-064992)

CAS 441798-33-0

Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.

Lasofoxifene tartrate

CAS 190791-29-8

Lasofoxifene Tartrate is a non-steroidal selective estrogen receptor modulator (SERM).

WAY 100635 Hydrochloride

CAS 146714-97-8

WAY 100635 Hydrochloride is available from DC Chemicals for laboratory research. Contact us for application-specific product information.

Atipamezole

CAS 104054-27-5

Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.

Filorexant(mk-6096)

CAS 1088991-73-4

Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).

Serotonin hydrochloride(5-HT)

CAS 153-98-0

Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.

Liothyronine sodium

CAS 55-06-1

3,3',5-Triiodo-L-thyronine sodium is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.

Israpafant

CAS 117279-73-9

Israpafant (Y24180) is a specific antagonist of PAF receptor that inhibits PAF-induced rabbit platelet aggregation in vitro (IC50=3.84 nM), with little effect on adenosine diphosphate- or arachidonic acid-induced aggregation.

Istradefylline (KW-6002)

CAS 155270-99-8

Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

Rupatadine

CAS 182349-12-8

Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).

BAN ORL 24

CAS 1401463-54-4

BAN ORL 24 is a potent and selective NOP receptor antagonist. (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively).

Bifeprunox

CAS 350992-10-8

Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of…

Timolol Maleate

CAS 26921-17-5

(S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).(S)-Timolol, 50% bioavailability following oral administration. Does not cross the blood brain…

FC131

CAS 606968-52-9

FC131 TFA is a CXCR4 antagonist that inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. FC131 TFA has anti-HIV activity.

pioglitazone hydrochloride

CAS 112529-15-4

For the detailed information of pioglitazone hydrochloride, the solubility of pioglitazone hydrochloride in water, the solubility of pioglitazone hydrochloride in DMSO, the solubility of pioglitazone hydrochloride in PBS buffer, the animal experiment（test）…

Acotiamide HCl

CAS 773092-05-0

Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic…

CTOP

CAS 103429-31-8

CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor…

VKGILS-NH2

CAS 942413-05-0

VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells[1][2].

Azilsartan medoxomil

CAS 863031-21-4

Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.

Retatrutide (LY3437943)

CAS 2381089-83-2

LY3437943 is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). LY3437943 inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79,…

NLX-101（F-15599）

CAS 635323-95-4

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.

Smoothened Agonist (SAG) HCl

CAS 2095432-58-7

SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.

BAY 2416964

CAS 2242464-44-2

BAY 2416964 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. AHR antagonist 3 has anti-cancer effects[1].

Risperidone(R 64 766)

CAS 106266-06-2

Risperidone(Risperdal) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism. This drug…

Pirmenol hydrochloride

CAS 61477-94-9

Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.

BTRX335140

CAS 2244614-14-8

BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.BTRX-335140 endows with favorable in vitro ADMET…

Gabapentin

CAS 60142-96-3

Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.

Trenbolone acetate

CAS 10161-34-9

Trenbolone acetate (RU-1697,17beta-TBOH) is a potent testosterone analog and selective androgen receptor modulator, is an androgen ester and a long-acting prodrug of trenbolone; shows SARM-like effects as it binds to androgen receptors (ARs) with…

Ozanimod hydrochloride

CAS 1618636-37-5

Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in 35S-GTPγS binding, respectively.

Methacholine Chloride

CAS 62-51-1

Methacholine chloride is used to constrict airway smooth muscle and to assess bronchial reactivity. Methacholine chloride is a cholinergic agonist and parasympathomimetic bronchoconstrictor. A metabolically stable analog of acetylcholine, it is a muscarin

Allopregnanolone

CAS 516-54-1

Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.

Elacestrant (dihydrochloride)

CAS 1349723-93-8

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

BEBT-809

BEBT-809 is a GPR75 antagonist for rat CYP4F2 and CYP4A11 with IC50 of and 15.76 nM and 33.16 nM, respectively.

Aripiprazole

CAS 129722-12-9

Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and…

Amisulpride

CAS 71675-85-9

Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. In Italy, it is also used as a treatment for dysthymia. It was introduced by Sanofi-Aventis in the 1990s. Its patent had expired by…

HTL0041178

CAS 2642079-89-6

HTL0041178 is a potent GPR52 agonist with EC50 of 27.5 nM (human or rat GPR52).

Indacaterol

CAS 312753-06-3

Indacaterol is a potent, orally administered ultra-long-acting β2 adrenergic receptor (ADRB2) agonist, widely recognized for its therapeutic potential in respiratory and cardiovascular conditions. By selectively activating ADRB2, indacaterol not only enhances…

SNC-80

CAS 156727-74-1

SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive,…

Desmopressin (Acetate)

CAS 62288-83-9

Desmopressin(DDAVP) acetate is the synthetic analogue of the antidiuretic hormone arginine vasopressin. IC50 Value:Target: Vasopressin ReceptorThe antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal…

Motixafortide(BKT140)

CAS 664334-36-5

BKT140 4-fluorobenzoyl is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM. Sequence: 4F-Benzoyl-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-Lys-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2(Disulfide bridge: Cys4-Cys13).