ADX 47273
CAS 851881-60-2
ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
GPCRs & Receptor Biology products
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Tretinoin(Retinoic acid）
CAS 302-79-4
Tretinoin(Retinoic acid） is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ…
Ibutamoren mesylate
CAS 159752-10-0
Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.
GSK3787
CAS 188591-46-0
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
DY131
CAS 95167-41-2
DY131, a selective ERRγ agonist, could potentiate the ERRγ-induced growth inhibition in LNCaP- ERRγ and DU145- ERRγ cells in a dose-dependent manner compared with respective parental cells. DY131 inhibited the growth of the ERα-positive endometrial cancer…
Ligandrol (VK5211, LGD-4033)
CAS 1165910-22-4
LGD-4033 is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity.
Smoothened Agonist (SAG) free base
CAS 912545-86-9
SAG is a potent Smo receptor agonist which activates the Hedgehog signaling pathway with a Kd of 59 nM.
Dexmedetomidine hydrochloride
CAS 145108-58-3
Dexmedetomidine, acting at alpha(2A) adrenoceptors, must be present during the encoding process to decrease discrete cue fear memory; however, its ability to suppress contextual memory is likely the result of blocking the consolidation process.…
Irbesartan
CAS 138402-11-6
Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.Target: Angiotensin ReceptorIrbesartan treatment markedly induces the expression of the adipogenic marker gene adipose protein 2 (aP2) in 3T3-L1…
Tiagabine hydrochloride
CAS 145821-59-6
Tiagabine hydrochloride(NO328 hydrochloride) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Tiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1…
GW-3965 hydrochloride
CAS 405911-17-3
GW3965 hydrochloride is a potent and selective LXR agonist with EC50s of 190 and 30 nM for hLXRα and hLXRβ , respectively.
GSK-0660
CAS 1014691-61-2
GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.
AMD3465
CAS 185991-07-5
AMD 3465 hexahydrobromide is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no…
Fexaramine
CAS 574013-66-4
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds. IC50 value:Target:in vitro: In vitro treatment of CDCA or fexaramine elevated the SHP transcript level and occupancy on secretin…
Vorapaxar Sulfate (SCH 530348)
CAS 705260-08-8
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide…
WIN-55212-2 mesylate
CAS 131543-23-2
WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
Fulvestrant
CAS 129453-61-8
Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.
Lorediplon
CAS 917393-39-6
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.Target: GABALorediplon is a drug for the treatment of insomnia, has been successfully…
Obeticholic acid (INT-747)
CAS 459789-99-2
INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.
Eplerenone
CAS 107724-20-9
Eplerenone is an aldosterone antagonist with an IC50 of 0.36 μM.Eplerenone is a selective mineralocorticoid receptor antagonist, which has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the…
WY14643 (Pirinixic Acid)
CAS 50892-23-4
Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
Capromorelin
CAS 193273-69-7
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
ODM-201(Darolutamide)
CAS 1297538-32-9
ODM-201 is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in AR-HEK293 cells.
Vipadenant
CAS 442908-10-3
Vipadenant is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
ML-224
CAS 1338824-21-7
ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.
Balixafortide(POL6326)
CAS 1051366-32-5
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and…
GW-627368X
CAS 439288-66-1
GW627368(GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).IC50 value: Target: EP4 antagonistin vitro: At recombinant human prostanoid EP4 receptors…
FFA4 (GPR120) agonist GSK137647A
CAS 349085-82-1
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.IC50 value: 6.3/6.2/6.1 (pEC50, for human/mouse/rat FFA4)Target: FFA4The pEC50s for Human , Mouse and Rat FFA1/2/3 are ＜ 4.5. GSK137647A is…
Eupatilin
CAS 22368-21-4
Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
AVN-492
CAS 1220646-23-0
AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
Lu AF21934
CAS 1445605-23-1
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
RG7090（Basimglurant）
CAS 802906-73-6
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
Emraclidine
CAS 2170722-84-4
Emraclidine is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases.
Plerixafor octahydrochloride
CAS 155148-31-5
Plerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.
GSK2981278
CAS 1474110-21-8
GSK2981278 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124.
(E/Z)-4-hydroxy Tamoxifen
CAS 68392-35-8
(E/Z)-4-Hydroxytamoxifen is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is an estrogen receptor modulator.
Afoxolaner
CAS 1093861-60-9
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions,…
BMS-204493
CAS 215030-90-3
BMS-204493(BMS493) is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation[1][2].
Taprenepag(CP-544326)
CAS 752187-80-7
CP-544326 is a potent and selective prostaglandin E2 receptor agonist with an EC50 of 2.8 nM.
BAF312 (Siponimod)
CAS 1230487-00-9
Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively.)
Pemafibrate
CAS 848259-27-8
Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 μM and 1.58 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively, and possesses lipid-lowering effect.
Bay 59-3074
CAS 406205-74-1
Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively . Orally active CB1 agonist in vivo.
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