Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12855 |
SB 258719
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
SB 258719 是高亲和力的、选择性的5-HT7受体拮抗剂,pKi 为7.5。SB 258719在癌症和神经系统疾病领域有研究价值。 | |||
T75720 |
Thrombospondin-1 (1016-1023) (human, bovine, mouse)
|
Apoptosis | Apoptosis |
Thrombospondin-1 (1016-1023) (human, bovine, mouse) 是 Thrombospondin-1 (TSP-1) 的一部分,是一种具有 CD47 激动作用的多肽。 | |||
T8706 |
STAMBP-IN-1
|
Others | Others |
STAMBP-IN-1是一种新型选择性去泛素酶 STAM 结合蛋白 (STAMBP) 拮抗剂,可降低 NALP7 蛋白水平并抑制 TLR 激动后 IL-1β 的释放。 | |||
T4093 |
Fabomotizole hydrochloride
Afobazole hydrochloride,CM346 hydrochloride |
MAO | Metabolism; Neuroscience |
Fabomotizole hydrochloride (CM346 hydrochloride) 是一种具有抗焦虑和神经保护作用的化合物。 | |||
TP1617L |
Chemerin-9 (149-157) acetate
Chemerin-9 (149-157) acetate (676367-27-4 free base) |
Others | Others |
Chemerin-9 (149-157) acetate (676367-27-4 free base) 对应于加工的 chemerin 的 C 末端,保留了全尺寸蛋白质的大部分活性和关于对 chemerinR 的激动。它是 ChemR23 (chemerinR) 的天然配体。 | |||
T36520 |
COR659
|
Cannabinoid Receptor; GABA Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。 | |||
T23794 |
BIO592
BIO-592,BIO 592 |
||
BIO592 is a modulator of RORγt. BIO592 triggers inverse agonism of RORγ. | |||
T23662 |
Aganodine
Aganodin |
||
Aganodine is a guanidine that activates presynaptic imidazoline receptors. Aganodine inhibits the presynaptic release of norepinephrine through its agonism at imidazoline receptors. | |||
T62722 |
SC13
|
||
SC13 是一种新型的 mitragynine 类似物,具有低效Muopioid receptor 激动作用,具有麻醉作用和较轻的不良反应。 | |||
T27489 |
GSK-7227
GSK7227,GSK 7227 |
||
GSK-7227, a novel class of PPARdelta partial agonists, shows potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells. | |||
TP1435 |
Chemerin-9 (149-157) TFA(676367-27-4 free base)
Chemerin-9 (149-157) (TFA) |
||
Chemerin-9 (149-157) TFA, the nonapeptide (149)YFPGQFAFS(157) (chemerin-9), corresponding to the C terminus of processed chemerin, retains most of the activity of the full-size protein, with regard to agonism toward the chemerinR[1]. | |||
T68881 |
OL-135
|
||
OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism. | |||
T16396 |
OP-3633
|
Others | Others |
OP-3633 is an effective and selective steroidal glucocorticoid receptor (GR) antagonist (IC50: 29 nM). OP-3633 shows low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism. It also has an inhibition of GR transcriptional activity. | |||
T70073 |
Fabomotizole dihydrochloride
|
||
Fabomotizole, also known as Afobazole, Obenoxazine and CM346, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be al... | |||
TP1617 |
Chemerin-9 (149-157)
Chemerin-9 149-157 |
||
The nonapeptide 149,YFPGQFAFS157 (chemerin-9), corresponding to the C terminus of processed chemerin, retained most of the activity of the full-size protein, with regard to agonism toward the chemerinR.the natural ligand of ChemR23 (chemerinR). | |||
T38199 |
(±)-WIN 55,212 (mesylate)
|
||
(±)-WIN 55,212-2 is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki value of 62.3 and 3.3 nM for human recombinant central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, respectively. In contrast, the enantiomer (-)-WIN 55,212-3 acts a partial inverse agonist at CB1 (pIC50 = 5.5) and as a competitive neutral antagonist of CB2, reversing the inverse agonism evoked by SR 144528 (pEC50 = 5.3). (+)-WIN 55,212 (mesylate) is a mixture of the two enantiomers, (+)-WI... | |||
T70379 |
PF-04479745 tartrate
|
||
PF-04479745, also known as PF-4479745, is a potent and selective 5-HT2C agonist (EC50 = 10 nM). PF-4479745 displayed robust pharmacology in a preclinical canine model of stress urinary incontinence (SUI) and no measurable functional agonism at the key selectivity targets 5-HT2A and 5-HT2B in relevant tissue-based assay systems. | |||
T80121 |
Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
|
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 是一种环状八肽,能够激活MC4R。该化合物能显著提高心率与血压。 | |||
T63514 | PPARγ agonist 1 | ||
PPARγ agonist 1 是 PPARγ 的有效激动剂,能够高效的激活 hPPARγ ,并不引起完全激动,进而能够避免不良反应。PPARγ agonist 1 对代谢紊乱相关心血管疾病表现出研究潜力。 | |||
T71707 |
Romergoline
|
||
Romergoline 是一种新合成的麦角碱衍生物,具有独特的药理作用,在正常动物中表现出完全的多巴胺(DA)拮抗作用,而在“去神经”动物模型中表现出完全的DA 拮抗作用。 | |||
T62554 | PPARγ phosphorylation inhibitor 1 | ||
PPARγ phosphorylation inhibitor 1 (Compound 10) 是一种有效的 PPARγ结合剂 (IC50: 24 nM),具有抗糖尿病效果。PPARγ phosphorylation inhibitor 1 对 CDK5 介导的 PPARγ Ser273 磷酸化表现出抑制作用 (IC50: 160 nM),且几乎无 PPARγ 激动作用。 | |||
T78779 |
D3R/MOR antagonist 2
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
D3R/MOR antagonist 2(Compound 121)为一种D3R/MOR拮抗剂,其Ki值分别为46.5 nM及691 nM。该化合物通过MOR部分激动作用可产生镇痛效果,并通过D3R拮抗减少阿片类药物的潜在滥用风险。 | |||
T71963 |
(−)-WIN 55,212-3 mesylate
|
||
(−)-WIN 55,212-3 mesylate is an aminoalkylindole derivative which acts as a competitive neutral antagonist of the human cannabinoid CB2 receptor, blocking both the stimulating action of CP 55,940 and the inverse agonism of SR 144528. (−)-WIN 55,212-3 neither antagonizes nor mimics the effects of Δ9-THC on rat cerebellar membranes, which presumably express the CB1 receptor. (−)-WIN 55,212-3 also weakly antagonizes the melatonin MT1 and muscarinic M4 receptors but has no effect on several other G ... | |||
T78778 |
D3R/MOR antagonist 1
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
D3R/MOR antagonist 1 (Compound 114) 为D3R/MOR拮抗剂,其对D3R和MOR的Ki值分别为46.5 nM和691 nM。该化合物通过MOR的部分激动作用可能具有镇痛效果,同时通过D3R的拮抗作用有助于降低阿片类药物的滥用风险。 | |||
T79547 |
MOR agonist-2
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
MOR agonist-2 (Compound 46) 为D3R拮抗剂及MOR激动剂,其Ki值分别为7.26 nM和564 nM。MOR agonist-2潜在以MOR部分激动机制实现镇痛效果,并通过D3R拮抗降低阿片类药物的滥用风险。 | |||
T81763 |
MOR agonist-3
|
||
MOR Agonist-3 (Compound 84) 是一种双重作用化合物,具有D3R/MOR拮抗活性(Ki值为55.2 nM和382 nM)。该化合物其MOR部分激动性质展现出镇痛潜力,并可能通通过D3R拮抗作用降低阿片类药物的滥用风险。MOR Agonist-3 亦适用于炎症治痈和神经性疼痛的研究领域。 | |||
T70077 |
Fadolmidine HCl
|
||
Fadolmidine, also known as MPV-2426, is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. Fadolmidine displayed high affinity and full agonist efficacy at all three human alpha2-adrenoceptor subtypes (A, B and C) in transfected CHO cells with EC50 values (nM) of 0.4, 4.9 and 0.5, respectively. Fadolmidine inhibited also electrically evoked contractions in rat vas deferens demonstrating the activation of rodent presynaptic alpha2D-adrenoceptors with an ... |