NS11394
CAS 951650-22-9
NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
GPCRs & Receptor Biology
G-protein-coupled, nuclear and other ligand-binding receptors and their modulators.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
GPCRs & Receptor Biology products
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Rolapitant
CAS 552292-08-7
Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
Pipequaline
CAS 77472-98-1
Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.
VU0357017
CAS 1135242-13-5
VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
Ciforadenant (CPI-444)
CAS 1202402-40-1
CPI-444 is a potent and selective inhibitor of A2A receptor (A2AR) induces antitumor responses.
AM 281
CAS 202463-68-1
AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].
Substance P free acid
CAS 71977-09-8
Substance P, Free Acid is a native substance P analog, but shows no biological activity of substance P.
Sitaxentan sodium
CAS 210421-74-2
Sitaxsentan (sodium) is an orally active, highly selective antagonist of endothelin A receptors.
Bazedoxifene
CAS 198481-32-2
Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.modulatorPreclinical and clinical studies with bazedoxifene demonstrate more tissue selectivity than other SERMs. In particular,…
GW0742
CAS 317318-84-6
GW0742 is a high affinity PPAR β/δ agonist with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
Cinacalcet (AMG-073) HCl
CAS 364782-34-3
Cinacalcet hydrochloride is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
RS 504393
CAS 300816-15-3
RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
MK-1064
CAS 1207253-08-4
MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.target: 2-SORA [1]In vivo: MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range…
NE-100
CAS 149409-57-4
NE-100 (hydrochloride) is a potent and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 (hydrochloride) exerts antipsychotic activity in vivo[1]. NE-100 (hydrochloride) also suppresses ER stress-induced hippocampal cell death[2].
SCH 23390 hydrochloride
CAS 125941-87-9
SCH 23390 hydrochloride is a potent dopamine receptor D1 antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5.
AZD4635
CAS 1321514-06-0
AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM.
TCS 1102
CAS 916141-36-1
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).TCS-1102 (10 and 20 mg/kg, i.p.) were found to decrease fear and anxiety in rats 14 days after exposure to footshock.Furthermore,…
Cilengitide (TFA salt)
CAS 199807-35-7
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
CID16020046
CAS 834903-43-4
CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM
rac BHFF
CAS 123557-91-5
rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor[1].
EPI-001
CAS 227947-06-0
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in…
Vorapaxar
CAS 618385-01-6
Vorapaxar is a protease-activated receptor (PAR-1) antagonist that inhibits thrombin-induced platelet activation.
Suvorexant
CAS 1030377-33-3
Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.
Liraglutide
CAS 204656-20-2
Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.
L-Stepholidine
CAS 16562-13-3
L-Stepholidine (Stepholidine), an alkaloid extract of the Chinese herb Stephania intermedia, is the first compound known to exhibit mixed dopamine D1 receptor agonist/D2 antagonist properties. L-Stepholidine (Stepholidine) has neuroprotective effect and…
Cyclobenzaprine HCl
CAS 6202-23-9
Cyclobenzaprine Hcl is a skeletal muscle relaxant and a central nervous system (CNS) depressant.Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine was thought to be an alpha 2-adrenoceptor agonist that…
ADX-88178
CAS 1235318-89-4
ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.
PF-3274167（cligosiban）
CAS 900510-03-4
Cligosiban (PF-3274167) is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.
Bepotastine Besilate
CAS 190786-44-8
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.
Cyclo(RGDfC)
CAS 862772-11-0
Cyclo (RGDfC), avb3 Integrin Binding Cyclic RGD Peptide,This is a cyclic RGDfC sequence, an integrin avb3-affine peptide.
LY-2940680(Taladegib)
CAS 1258861-20-9
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
Devazepide
CAS 103420-77-5
Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.
Olodanrigan(EMA401)
CAS 1316755-16-4
Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
AZD2098
CAS 566203-88-1
AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.
Degarelix (acetate)
CAS 214766-78-6
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
Fevipiprant
CAS 872365-14-5
Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human…
PF04995274,PF 04995274
CAS 1331782-27-4
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat…
Xanthine amine congener
CAS 96865-92-8
Xanthine amine congener (XAC) is a non-selective adenosine receptor antagonist with Kb values of 83, 25, and 15 nM for rat PC12 cells, human platelets that endogenously express adenosine A2A receptors, and rat fat cells that endogenously express A1 recept
CGP-71683A
CAS 192322-50-2
CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
Balaglitazone
CAS 199113-98-9
Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
APD668
CAS 832714-46-2
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.Chronic treatment withAPD668 showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker…
Guanoclor
CAS 5001-32-1
Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.
MRE-269
CAS 475085-57-5
MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
ONO-7300243
CAS 638132-34-0
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
GDC-0810
CAS 1365888-06-7
GDC-0810 is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
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