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.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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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.
Varenicline
CAS 249296-44-4
Varenicline(CP 526555;Champix) is a selective α4β2 nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.Varenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking…
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.
KN-62
CAS 127191-97-3
KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
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.…
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.
CZC-25146
CAS 1191911-26-8
CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.
CGS 21680 hydrochloride
CAS 124431-80-7
CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
NS638
CAS 150493-34-8
NS-638 is a small nonpeptide molecule with Ca2+-channel blocking properties. K+-stimulated intracellular Ca2+-elevation is blocked with an IC50 value of 3.4 μM.
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…
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].
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 =…
DAA1106
CAS 220551-92-8
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.Target:PBRin vitro: DAA1106 binding to PBR was significantly increased in widespread areas in…
Fluoroclebopride
CAS 154540-49-5
Fluoroclebopride is useful chemical for PET image study. [18F]fluoroclebopride had been used for PET imaging of dopamine D2 receptors in monkeys
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…
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.
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.
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.
DAPT
CAS 208255-80-5
DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.
α-Amyloid Precursor Protein Modulator(TPPB)
CAS 497259-23-1
α-Amyloid Precursor Protein Modulator(TPPB) is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.
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].
(-)MK-801 maleate
CAS 121917-57-5
(-)-MK 801 Maleate is the enantiomer of (+)-MK-801. (+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist.
(+)MK-801 maleate
CAS 77086-22-7
(+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
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.
DNQX
CAS 2379-57-9
DNQX is a AMPA receptor antagonists.target: AMPA receptorIn vitro: DNQX, added 2 h after cell plating, induces a dose-dependent neurotoxicity.
CNQX disodium salt
CAS 479347-85-8
CNQX is a potent AMPA/kainate receptor antagonist. Also antagonist at glycine modulatory site on NMDA receptor complex.
DNQX disodium salt
CAS 1312992-24-7
DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively)[1].
Verubecestat (MK-8931)
CAS 1286770-55-5
Verubecestat (MK-8931) is a beta-secretase 1 (BACE1) inhibitor under investigation for the treatment of Alzheimer's Disease.
VX-745
CAS 209410-46-8
Neflamapimod (VX-745) is a potent and selective inhibitor of p38α, and possesses anti-inflammatory activity.
SB-705498
CAS 501951-42-4
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
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,…
SB-366791
CAS 472981-92-3
SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nM. SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis…
Tat-NR2B9c
CAS 500992-11-0
Tat-NR2B9c is a 20-aa peptide, which acts as a postsynaptic density-95 (PSD-95) inhibitor, with an EC50 of 6.7 nM for PSD-95d2 (PSD-95 PDZ domain 2), and 670 nM for PSD-95d1; Tat-NR2B9c also reduces NMDA-induced p38 activation, and possesses neuroprotective…
DS-1971a
CAS 1450595-86-4
DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects[1].
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