BMY 7378
CAS 21102-95-4
BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
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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Sertindole
CAS 106516-24-9
Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative…
GRA Ex-25
CAS 307983-31-9
GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
PSB-16671
CAS 2094630-35-8
PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays. PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor. PSB-16671 shows an EC50 of…
GSK-805
CAS 1426802-50-7
GSK805, also known as ROR gamma-t-IN-1, is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.
IPSU
CAS 1373765-19-5
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
SR 8278
CAS 1254944-66-5
SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm[1][2].
Icatibant
CAS 130308-48-4
Icatibant is a peptidomimetic drug consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. It has been approved by the European Commission for the symptomatic treatment of acute attacks of hereditary angioedema…
Zuranolone
CAS 1632051-40-1
Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor.
Intepirdine (SB-742457, RVT-101）
CAS 607742-69-8
SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.SB-742457, a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic…
SR9011
CAS 1379686-29-9
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
Ralinepag
CAS 1187856-49-0
Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
Apalutamide（ARN509）
CAS 956104-40-8
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
Cangrelor free acid
CAS 163706-06-7
Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate.…
Rimonabant(SR141716)
CAS 168273-06-1
Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
BD1047.2HBr
CAS 138356-21-5
BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
CID 1375606
CAS 313493-80-0
CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
Tropifexor (LJN452)
CAS 1383816-29-2
Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
AZD1981
CAS 802904-66-1
AZD1981 is a potent and selective CRTh2 antagonist; displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).
TAK-071
CAS 1820812-16-5
TAK-071 is a novel muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM[1].
DANUGLIPRON（PF-06882961）
CAS 2230198-02-2
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R)
BAR 502
CAS 1612191-86-2
BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
BMS813160
CAS 1286279-29-5
BMS-813160 is the first dual CCR2/CCR5 antagonist to enter clinical development for cardiovascular.
Pasireotide
CAS 396091-73-9
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
LXRβ agonist 17
CAS 1878259-00-7
A novel, potent, orally active liver X receptor β (LXRβ) agonist with Ki/EC50 of 3/21 nM, displays 27-fold selectivity over LXRα; also exhibits excellent selectivity against other nuclear hormone receptors (>3,000-fold); induces the expression of LXR target…
GR-127935 hydrochloride
CAS 148642-42-6
GR-127935 potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.
Pitolisant (hydrochloride)
CAS 903576-44-3
Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
AM095
CAS 1345614-59-6
AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively. AM095 is an LPA1 receptor antagonist with good oral exposure and antifibrotic activity in rodent models. In vitro, AM095…
Atosiban
CAS 90779-69-4
Atosiban(RW22164; Tractocile) is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane.As a…
Eluxadoline
CAS 864821-90-9
Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist. in vitro: Eluxadoline is a locally active, mixed ?-opioid receptor (?OR) agonist and δ-opioid receptor (δOR) antagonist being developed for the treatment…
MK-0557
CAS 328232-95-7
MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
PrNMI
CAS 1541244-33-0
PrNMI is a peripherally restricted cannabinoid 1 receptor (CB1R) agonist, significantly alleviates spontaneous pain behaviors in the animals.
AZD9496
CAS 1639042-08-2
AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM.
Sparsentan(PS433540)
CAS 254740-64-2
Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Levobetaxolol hydrochloride
CAS 116209-55-3
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.
N-Desmethylclozapine
CAS 6104-71-8
N-Desmethylclozapine is a dengue virus inhibitor, and an agonist of δ-opioid receptor.
ORM-15341(Ketodarolutamide)
CAS 1297537-33-7
ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.IC50 value: 38…
AT-56
CAS 162640-98-4
AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2[1].
JNJ-10229570
CAS 524923-88-4
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells…
LY2795050
CAS 1346133-08-1
LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]Target: κ-opioid Receptorin vitro: LY2795050 displays…
WAY 100635 maleate salt
CAS 634908-75-1
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ± 0.12 nM for 5-HT.
Treprostinil free acid
CAS 81846-19-7
Treprostinil is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
Namodenoson (CF-102)
CAS 163042-96-4
Namodenoson (CF-102) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
Alcaftadine
CAS 147084-10-4
For the detailed information of Alcaftadine, the solubility of Alcaftadine in water, the solubility of Alcaftadine in DMSO, the solubility of Alcaftadine in PBS buffer, the animal experiment（test） (test) of Alcaftadine, the cell expriment (test) of…
Cangrelor sodium
CAS 163706-36-3
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and…
CYN 154806
CAS 183658-72-2
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively[1][2].
EDP-305
CAS 1933507-63-1
EDP-305 is a novel and potent farnesoid X receptor (FXR) agonist, with no/minimal cross-reactivity to TGR5 or other nuclear receptors.
MRS1754
CAS 264622-58-4
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats[1].
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