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Pam2CSK4 (TFA), a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 (TFA) promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 (TFA) also activates iNOS expression and NO production in mouse macrophages .
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
Pam3Cys-Ser-(Lys)4 trihydrochloride is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages .
PAM Human Pre-designed siRNA Set A contains three designed siRNAs for PAM gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PAM16 Human Pre-designed siRNA Set A contains three designed siRNAs for PAM16 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Polyacrylamide,Anion,Mw 18 million (PAM,Anion,Mw 18 million) can be used to synthesize water-soluble polymers. Polyacrylamide,Anion,Mw 18 million is a biomaterial or organic compound that can be used as a biomaterial or organic compound related to life science research .
Polyacrylamide,Anion,Mw 14-16 million (PAM,Anion,Mw 14-16 million) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Polyacrylamide,Anion,Mw 10-12 million (PAM,Anion,Mw 10-12 million) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Polyacrylamide, average Mn 150000 (PAM, average Mn 150000) is a multifunctional polymer with moisturizing properties. Polyacrylamide,average Mn 150000 is a kind of biological materials or organic compounds that are widely used in life science research .
Polyacrylamide, average Mn 40000 (PAM, average Mn 40000) is a multifunctional polymer with moisturizing properties. Polyacrylamide,average Mn 40000 is a kind of biological materials or organic compounds that are widely used in life science research .
CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .
Pralidoxime chloride is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime chloride reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime chloride is an antidote for organophosphate poisoning .
VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses .
MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7?μM for Pam3CSK4-induced hTLR2/1 and 5.7?μM for Pam2CSK4-induced hTLR2/6 responses .
VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively .
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4?PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs .
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .
CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM .
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB?of 6.02 (～1?μM). BMS-986187 has no observable PAM activity at the?μ-receptor (EC50=3 μM) .
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases .
VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia .
Z8554052021 (compound 2021) is a potent CaSR and indeed GPCR positive allosteric modulator (PAM) with an EC50 of 3.3 nM. Z8554052021 has the potential for hyperparathyroidism research .
JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo .
AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases .
Gentisuric acid, a metabolite of Aspirin (HY-14654), is a substrate of α-amidating monooxygenase (PAM). Gentisuric acid prevents DNA-damage by Mitomycin C (HY-13316) .
LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4PAM) with an EC50 of 79 nM . Antiparkinsonian effect .
VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .
VU6008677 is a positive allosteric modulator (PAM) for M4, with EC50 of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats .
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM .
VU0366369 (ML137) is a selective positive allosteric modulator (PAM) for mAChR M1 with an EC50 of 830 nM. VU0366369 can be used in research about central nervous system diseases .
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor
positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM) .
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4PAM) , with an EC50 of 79 nM . Antiparkinsonian effect .
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenous ligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC50 of 3.2 μM .
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50?= 7.71) .
Nampt activator-4 is a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of 0.058 μM. Nampt activator-4 can enhance the nicotinamide adenine dinucleotide (NAD +) in cells .
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .
VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease .
VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities .
TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity .
VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
V-0219 hydrochloride (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 hydrochloride can be used for obesity-associated diabetes research .
V-0219 (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 can be used for obesity-associated diabetes research .
VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .
MB327 is a bipyridine nonoxime compound that restores neuromuscular function. MB327 restores the activity of nicotinamide acetylcholine receptors (nAChRs) for carbachol desensitization in a typical type II PAM manner. MB327 can neutralize nerve agent poisoning .
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders .
UBP714 exhibts agonistic activity for recombinant GluN1/GluN2 receptor by binding to the positive allosteric site (PAM) of NMDARs. UBP714 enhances NMDAR-mediated field excitatory postsynaptic potentials (f-EPSPs) in Xenopus oocytes .
VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain .
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70 .
VU0119498 is a pan GqmAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity .
α7 nAChR Modulator-2 (Compound 7b) is a α7 nAChR positive allosteric modulator (PAM) with an EC50 of 2.1 μM. α7 nAChR Modulator-2 can be used for the research of cognitive disorders .
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
BIO-2007817 is a Parkin positive allosteric modulators (PAMs). BIO-2007817 enhances the activity of wildtype Parkin. BIO-2007817 stimulates Parkin (an E3 ligase)autoubiquitination and induces the appearance of monoubiquitinated forms of Miro1 (EC50: 0.17 μM) .
VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders .
(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders .
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
GABAA receptor modulator-3 (compound 3b) is a positive allosteric modulator (PAM). GABAA receptor modulator-3 inhibits α1β3γ2 GABAAR at peak and steady state currents with IC50s of 671 and 64 μM, respectively .
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research .
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research .
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
(R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R .
(R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R .
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .
MCUF-651 is an orally active guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM) (KD: 397 nM ). MCUF-651 binds to GC-A and selectively enhances the binding of atrial natriuretic peptide (ANP) to GC-A. MCUF-651 enhances ANP-mediated cGMP generation in human cardiac, renal, and fat cells. MCUF-651 inhibits cardiomyocyte hypertrophy .
Levamisole (Standard) is the analytical standard of Levamisole. This product is intended for research and analytical applications. Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells .
(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
GAT229 is a CB1 positive allosteric modulator (PAM) that effectively reduces intraocular pressure (IOP) in high IOP mouse models and enhances CB1 receptor-mediated IOP-lowering effects. A 0.2% GAT229 solution or 10 mg/kg of GAT229 alone significantly reduces IOP. GAT229 is promising for research related to glaucoma and elevated intraocular pressure .
(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders .
(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD) .
VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice .
(S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
(R,R,S)-GAT107 is a fully agonistic positive modulator of α7 nicotinic receptors with significant biological activity. Its activity is entirely present in its (+)-isomer 1b, while (-)-isomer 1a does not affect its activity when used together. Studies have shown that (R,R,S)-GAT107 is the most potent ago-PAM for α7 nicotinic receptors currently known and has the potential for further in vivo evaluation .
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity .
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 201 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
Polyacrylamide,Anion,Mw 18 million (PAM,Anion,Mw 18 million) can be used to synthesize water-soluble polymers. Polyacrylamide,Anion,Mw 18 million is a biomaterial or organic compound that can be used as a biomaterial or organic compound related to life science research .
Polyacrylamide,Anion,Mw 14-16 million (PAM,Anion,Mw 14-16 million) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Polyacrylamide,Anion,Mw 10-12 million (PAM,Anion,Mw 10-12 million) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Pam3Cys-Ser-(Lys)4 trihydrochloride is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Polyacrylamide, average Mn 150000 (PAM, average Mn 150000) is a multifunctional polymer with moisturizing properties. Polyacrylamide,average Mn 150000 is a kind of biological materials or organic compounds that are widely used in life science research .
Polyacrylamide, average Mn 40000 (PAM, average Mn 40000) is a multifunctional polymer with moisturizing properties. Polyacrylamide,average Mn 40000 is a kind of biological materials or organic compounds that are widely used in life science research .
Pam2CSK4 (TFA), a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 (TFA) promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 (TFA) also activates iNOS expression and NO production in mouse macrophages .
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
Pam3Cys-Ser-(Lys)4 trihydrochloride is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages .
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
The PAM protein is a bifunctional enzyme that coordinates the α-amidation process, which is critical for the biosynthesis of neuropeptides and endocrine peptides. The peptidyl α-hydroxylating monooxygenase (PHM) domain hydroxylates the C-terminal glycine, and the peptidylglycine amide glycolate lyase (PAL) domain cleaves the NC-α bond, producing α-amidated peptides. PAM Protein, Human (HEK293, His) is the recombinant human-derived PAM protein, expressed by HEK293 , with C-His labeled tag.
The JAM-A/CD321 protein is critical for the formation of tight junctions in epithelial cells, participating in early junction development and recruiting PARD3. However, the formation of PARD6-PARD3 complex may hinder PARD3-JAM1 interaction, thus preventing tight junction assembly. JAM-A/CD321 Protein, Rat (HEK293, His) is the recombinant rat-derived JAM-A/CD321 protein, expressed by HEK293 , with C-His labeled tag. The total length of JAM-A/CD321 Protein, Rat (HEK293, His) is 212 a.a., with molecular weight of 25 & 28 kDa, respectively.
The JAM-A/CD321 protein is critical for the formation of epithelial tight junctions, is present in early junction development, and recruits PARD3. Binding of the PARD6-PARD3 complex may hinder PARD3-JAM1 interaction, thereby impeding tight junction assembly. JAM-A/CD321 Protein, Human (HEK293, His) is the recombinant human-derived JAM-A/CD321 protein, expressed by HEK293 , with C-6*His labeled tag.
The PAM protein is a bifunctional enzyme that coordinates the α-amidation process, which is critical for the biosynthesis of neuropeptides and endocrine peptides. The peptidyl α-hydroxylating monooxygenase (PHM) domain hydroxylates the C-terminal glycine, and the peptidylglycine amide glycolate lyase (PAL) domain cleaves the NC-α bond, producing α-amidated peptides. PAM Protein, Human (HEK293, Fc) is the recombinant human-derived PAM protein, expressed by HEK293 , with C-hFc labeled tag.
The TIM-14 protein is an important component of the PAM complex and is required for the transport of transit peptide-containing proteins from the inner membrane to the mitochondrial matrix using ATP. TIM-14 Protein, S.cerevisiae is the recombinant TIM-14 protein, expressed by E. coli , with tag free. The total length of TIM-14 Protein, S.cerevisiae is 70 a.a., with molecular weight of ~9.0 kDa.
TIM-16 protein is an important component of the PAM complex, which uses ATP to promote the transfer of transit peptide-containing proteins from the inner membrane to the mitochondrial matrix. TIM-16 Protein, S. cerevisiae is the recombinant TIM-16 protein, expressed by E. coli , with tag free. The total length of TIM-16 Protein, S. cerevisiae is 66 a.a., with molecular weight of ~11.0 kDa.
The JAM-A/CD321 protein is critical for the formation of epithelial tight junctions and is present at primitive cell junctions where it recruits PARD3.This association may hinder PARD3-JAM1 interaction and thus tight junction assembly.JAM-A/CD321 Protein, Mouse (HEK293, His) is the recombinant mouse-derived JAM-A/CD321 protein, expressed by HEK293 , with C-His labeled tag.
The JAM-A/CD321 protein is critical for the formation of tight junctions in epithelial cells, participating in early junction development and recruiting PARD3. However, the formation of PARD6-PARD3 complex may hinder PARD3-JAM1 interaction, thus preventing tight junction assembly. JAM-A/CD321 Protein, Rat (HEK293, Fc) is the recombinant rat-derived JAM-A/CD321 protein, expressed by HEK293 , with C-hFc labeled tag.
The JAM-A/CD321 protein is critical for the formation of epithelial tight junctions and is present at primitive cell junctions where it recruits PARD3.This association may hinder PARD3-JAM1 interaction and thus tight junction assembly.JAM-A/CD321 Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived JAM-A/CD321 protein, expressed by HEK293 , with C-hFc labeled tag.
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
Junctional Adhesion Molecule 1 Antibody (YA3025) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3025), targeting Junctional Adhesion Molecule 1, with a predicted molecular weight of 33 kDa (observed band size: 33 kDa). Junctional Adhesion Molecule 1 Antibody (YA3025) can be used for WB, ICC/IF, IP experiment in human background.
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4?PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .
PAM Human Pre-designed siRNA Set A contains three designed siRNAs for PAM gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PAM16 Human Pre-designed siRNA Set A contains three designed siRNAs for PAM16 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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