SANT-1
CAS 304909-07-7
SANT-1 is a potent Smo antagonist, inhibits Hedgehog signaling, with IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively[1].
GPCRs & Receptor Biology
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
GPCRs & Receptor Biology products
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Olodaterol(BI-1744) hydrochloride
CAS 869477-96-3
Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary…
Finerenone
CAS 1050477-31-0
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and…
R(+)-Etomoxir (sodium salt)
CAS 828934-41-4
(R)-Etomoxir sodium salt is the R-form of Etomoxir sodium salt, acts as an inhibitorof carnitine palmitoyltransferase I (CPT-I), and inhibits palmitate β-oxidation in human, rat and guinea pig.
ML-18
CAS 1422269-30-4
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
Fosaprepitant dimeglumine
CAS 265121-04-8
Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Sarpogrelate (hydrochloride)
CAS 135159-51-2
Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have…
Asimadoline (EMD-61753)
CAS 153205-46-0
Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.
Cebranopadol(GRT-6005)
CAS 863513-91-1
Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
Desogestrel
CAS 54024-22-5
Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP).
Aclidinium bromide
CAS 320345-99-1
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
TC-O 9311
CAS 444932-31-4
TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM[1].
TUG-770
CAS 1402601-82-4
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
Ozanimod (RPC1063)
CAS 1306760-87-1
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.
Eltrombopag (SB-497115-GR)
CAS 496775-61-2
Eltrombopag is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.
CH-223191
CAS 301326-22-7
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 blocks the binding of TCDD to AhR with an IC50 of 0.03 µM.
Preladenant(SCH420814)
CAS 377727-87-2
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
TUG891
CAS 1374516-07-0
TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4.
VU-0357121(VU0357121)
CAS 433967-28-3
VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.
CERC-501(LY-2456302,Aticaprant)
CAS 1174130-61-0
LY-2456302 is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
Aprepitant (MK-0869, L-754030)
CAS 170729-80-3
Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
BMS-986020
CAS 1257213-50-5
BMS-986020 is an LPA1 antagonist.target: LPA1BMS-986020 is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic…
E-7046
CAS 1369489-71-3
E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.
CYM5442
CAS 1094042-01-9
CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442…
Etrasimod(APD334)
CAS 1206123-37-6
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
LY-404039
CAS 635318-11-5
LY404039 is an inhibitor for mGluR1(Ki=149 nM) and mGluR2(Ki= 92 nM), which can also inhibit dopamine receptor.Metabotropic glutamate (mGlu) receptors have been shown to mediate a number of behaviors including emotionality and responsivity to stress as…
Saclofen
CAS 125464-42-8
Saclofen is a competitive antagonist of the GABAB receptor with an IC50 of 7.8 μM. Saclofen can be used to determine the functional roles for the GABAB receptor as a mediator of slow inhibitory postsynaptic potentials in the brain[1].
CFMTI
CAS 864864-17-5
CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM. The selectivity of CFMTI to mGluR1 over mGluR5 was >2000-fold.
LY310762
CAS 192927-92-7
LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.IC50 value: 249 nM (Ki) [1]Target: 5-HT1D in vitro: LY310762 has a higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor.…
TTNPB
CAS 71441-28-6
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
VU 0364770
CAS 61350-00-3
VU0364770 is an allosteric of metabotropic glutamate receptor 4 (mGlu4) modulator, which exhibits a EC50 of 1.1±0.2 μM at human mGlu4.
CGS 21680 hydrochloride
CAS 124431-80-7
CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
Eptapirone
CAS 179756-58-2
F 11440 is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.Target: 5-HT1AThe affinity of F 11440 for 5-HT1Abinding sites (pKi, 8.33) was higher than that of buspirone (pKi , 7.50), and somewhat…
NIBR189
CAS 1599432-08-2
NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).NIBR189 is a potent and selective EBI2 antagonist with improved pharmacokinetic properties which will…
MSX-122
CAS 897657-95-3
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
RS-127445
CAS 199864-87-4
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites[1].
Imidafenacin
CAS 170105-16-5
Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).IC50 value: 0.3 nM(M3) [1]in vitro: KRP-197 showed equipotent anti-M2 and anti-M3 activity and decreased…
pardoprunox (SLV308)
CAS 269718-84-5
Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA =…
TG6-10-1
CAS 1415716-58-3
TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.
JNJ-63533054
CAS 1802326-66-4
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.IC50 value: 16 nM (EC50)Target: hGPR139in vitro: JNJ-63533054 is a selective small-molecule agonist. JNJ-63533054 specifically activates human GPR139 in the calcium mobilization…
AMG-837
CAS 865231-46-5
AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to…
Pimavanserin(ACP-103)
CAS 706779-91-1
Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
AL 082D06(D-06)
CAS 256925-03-8
AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
Fluralaner
CAS 864731-61-3
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
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