309
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4351 |
DAMGO
Dagol,DAGO,RX-783006 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
DAMGO (DAGO) 是一种阿片受体激动剂,Kd 值为 3.46 nM。它能够影响啮齿动物的运动活动,可作为镇痛剂。 | |||
T8991 |
BMS986187
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
BMS986187 是一种有效的δ-阿片受体选择性正变构调节剂 (PAM),其 EC50= 0.03 μM,pKB= 6.02 (~1 μM)。BMS986187 对 μ 受体无明显 PAM 活性 (EC50=3 μM)。 | |||
T1242 |
Alvimopan
爱维莫潘 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Alvimopan (LY 246736) 是一种选择性和竞争性 μ 阿片受体拮抗剂,IC50值为 1.7 nM。它存在于肌间和黏膜下神经元以及人体肠道固有层的免疫细胞中,可用于术后肠梗阻的研究。 | |||
T4691 |
Asimadoline hydrochloride
EMD-61753 hydrochloride,阿西马朵林盐酸盐 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Asimadoline hydrochloride (EMD-61753 hydrochloride) 是一种 κ-阿片(κ-opioid)受体激动剂,对豚鼠和人重组 κ-opioid 的 IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛,具有外周抗炎作用,并有用于肠易激综合征的研究潜力。 | |||
T62025 | μ opioid receptor agonist 2 | ||
μ opioid receptor agonist 2 (Compound H-3)是一种MOR 受体激动剂,可用于疼痛及疼痛相关疾病的研究。 | |||
T79430 | μ opioid receptor agonist 3 | Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
μopioid receptor agonist3 (compound 20) 是高效的μOR激动剂,其EC50 值为0.87 nM。该化合物在疼痛和神经精神适应症研究中具备潜在应用价值。 | |||
T62268 | μ opioid receptor agonist 1 | ||
μ opioid receptor agonist 1 (Compound H-1a)是一种光学纯的氧杂环取代吡咯并吡唑衍生物,也是一种 MOR 受体激动剂,能够用于研究疼痛及疼痛相关疾病。 | |||
T61901 |
σ1 Receptor/μ Opioid receptor modulator 1
|
||
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) 是一种有效的σ1受体拮抗剂(Ki= 1.86 nM)和μ阿片受体激动剂(Ki=2.1 nM)。σ1 Receptor/μ Opioid receptor modulator 1 具体有效的镇痛活性,可用于神经性疼痛的研究。 | |||
T78646 |
Estrogen receptor antagonist 8
|
Estrogen/progestogen Receptor | Endocrinology/Hormones |
Estrogen receptor antagonist 8 作为一种雌激素受体(ER)拮抗剂,具有抗子宫活性和潜在的抗肿瘤活性,可用于研究卵巢功能障碍。 | |||
T21620 |
Adenosine receptor antagonist 4
|
Adenosine Receptor | GPCR/G Protein; Neuroscience |
Adenosine receptor antagonist 4 是一种腺苷受体拮抗剂。 | |||
T5586 |
cFMS Receptor Inhibitor II
|
c-Fms | Tyrosine Kinase/Adaptors |
cFMS Receptor Inhibitor II 是 CSF-1R 激酶抑制剂。其中 CSF-1 是细胞因子。 | |||
T9247 |
Vanilloid receptor antagonist 1
4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile |
TRP/TRPV Channel | Membrane transporter/Ion channel |
Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) 是香草酸受体的有效拮抗剂。 | |||
TP1422 |
Interleukin (IL)-6 Receptor
|
Others | Others |
Interleukin (IL)-6 Receptor 是一种肽,来源于白细胞介素6受体。 | |||
T3177 |
Orexin 2 Receptor Agonist
OX2R |
OX Receptor | GPCR/G Protein; Neuroscience |
Orexin 2 Receptor Agonist (OX2R) 是一种选择性有效的OX2R 激动剂, EC50为23 nM。 | |||
T11349 |
GABAA receptor agent 1
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
GABAA receptor agent 1 是GABAA 受体的高亲和力配体,有抗惊厥活性。 | |||
T9244 |
σ1 Receptor antagonist-1
|
Sigma receptor | GPCR/G Protein |
σ1 Receptor antagonist-1 是高选择性的 sigma 1受体拮抗剂,pKi 为10.28。它抑制细胞生长,在 G0/G1 期阻滞细胞周期并诱导 MCF-7/ADR 细胞凋亡。 | |||
T13736 |
Interferon receptor inducer-1
|
IFNAR | Immunology/Inflammation |
Interferon receptor inducer-1 是一种干扰素(IFN)受体诱导剂,可用于干扰素诱导参与的紊乱性疾病的研究。 | |||
T4312 |
GPR120 Agonist 2
GPR120 receptor agonist |
GPR | Endocrinology/Hormones; GPCR/G Protein |
GPR120 Agonist 2 是一种选择性 GPR120激动剂。 | |||
T37734 |
AMPA receptor modulator-2
|
GluR | Neuroscience |
AMPA receptor modulator-2 是 AMPA 受体的有效调节剂,在 TARPγ2 依赖性 AMPA 受体上的pIC50为 10.1。 | |||
T37792 |
A2A receptor antagonist 1
CPI-444 analog,A2A receptor antagonist 1 |
Adenosine Receptor | GPCR/G Protein; Neuroscience |
A2A receptor antagonist 1 (CPI-444 analog)是腺苷 A2A 和 A1受体的拮抗剂,Ki 值分别为4和264 nM。 | |||
T12912 |
Sigma-1 receptor antagonist 3
|
Sigma receptor; HER | Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Sigma-1 receptor antagonist 3 是 Sigma-1受体选择性拮抗剂,Ki 为 1.14 nM。它抑制 hERG,IC50为 1.54μM。它在神经性疼痛方面有研究的价值。 | |||
T10058 |
A2B receptor antagonist 1
|
Adenosine Receptor | GPCR/G Protein; Neuroscience |
A2B receptor antagonist 1 是一个有效的 A2B 腺苷受体 (A2B adenosine receptor) 拮抗剂。 | |||
T22466 |
Adenosine receptor A1 antagonist 5
|
cAMP | GPCR/G Protein |
Adenosine receptor A1 antagonist 5 可作为一种腺苷拮抗剂,是一种氧嘌呤,可作为杀虫剂和虫害防治剂,对血压升高有抑制作用。 | |||
T4521 |
Edg-2 receptor inhibitor 1
SAR-100842 |
LPA Receptor | GPCR/G Protein |
Edg-2 receptor inhibitor 1 (SAR-100842) 是一种提取的 Edg-2 受体抑制剂 (IC50: <0.1 μM)。 | |||
T11211 |
EP4 receptor antagonist 1
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
EP4 receptor antagonist 1 是一种有效的特异性前列腺素 EP4受体拮抗剂,对人和小鼠 EP4受体的 IC50分别为6.1 nM 和16.2 nM。 EP4 receptor antagonist 1 可用于癌症免疫治疗的研究。 | |||
T5829 |
H4 Receptor antagonist 1
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
H4 Receptor antagonist 1 是选择性组胺 H4受体反向激动剂,其IC50值为19 nM。 | |||
T12910 |
Sigma-1 receptor antagonist 1
|
Sigma receptor | GPCR/G Protein |
Sigma-1 receptor antagonist 1 是一种有效、特异性的 sigma-1 受体拮抗剂。 Sigma-1 receptor antagonist 1 具有抗神经性疼痛活性,可用于治疗神经性疼痛研究。 | |||
T12911 |
Sigma-1 receptor antagonist 2
|
Sigma receptor | GPCR/G Protein |
Sigma-1 receptor antagonist 2 是有效的sigma 1受体选择性拮抗剂,与 σ1 和 σ2 受体结合的Ki 分别为 3.88 和 1288 nM。 | |||
T10250 |
ADRA1D receptor antagonist 1 HCl
ADRA1D receptor antagonist 1 HCl(1191908-24-3 free base) |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
ADRA1D receptor antagonist 1 HCl 是一种具有口服活性、高效性和选择性的 α1D 肾上腺素受体拮抗剂(Ki:1.6 nM),具有潜在的抗增殖活性。 | |||
TP1704 |
Galanin Receptor Ligand M35 TFA
|
Neuropeptide Y Receptor | GPCR/G Protein; Neuroscience |
Galanin Receptor Ligand M35 TFA(142846-71-7 free base) 是一种高亲和力配体和甘丙肽受体拮抗剂 (Kd=0.1 nM)。 | |||
T9579L |
GLP-1 receptor agonist 9 citrate
GLP-1 receptor agonist 9 citrate (2401892-71-3 Free base) |
Glucagon Receptor | GPCR/G Protein |
GLP-1 receptor agonist 9 citrate 是 GLP-1 的激动剂。 | |||
T4031 |
S1p receptor agonist 1
S1p-receptor-agonist-1 |
S1P Receptor; LPL Receptor | GPCR/G Protein |
S1p receptor agonist 1 (S1p-receptor-agonist-1) 是有口服活性的S1P 受体激动剂,具有诱导 S1P1 内化的活性,EC50为9.83 nM。它有潜力用于关节炎和实验性自身免疫性脑炎)的相关研究。 | |||
T60075 |
Dopamine D2 receptor agonist-2
Dopamine D2 Receptor |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) 是靶向多巴胺D2受体的配体。 | |||
T14127 |
Adenosine A1 receptor activator T62
|
Adenosine Receptor | GPCR/G Protein; Neuroscience |
Adenosine A1 receptor activator T62 是腺苷 A1 受体的变构增强剂,有镇痛作用。 | |||
T4633 |
Asimadoline
EMD-61753,阿西马朵林 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Asimadoline (EMD-61753) 是一种 κ-阿片(κ-opioid)受体激动剂,对豚鼠和人重组 κ-opioid 的IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛,具有外周抗炎作用,并有用于肠易激综合征的研究潜力。 | |||
T38836L |
Protease-Activated Receptor-1, PAR-1 Agonist acetate
|
Protease-activated Receptor | GPCR/G Protein |
Protease-Activated Receptor-1, PAR-1 Agonist acetate 是一种选择性蛋白酶激活受体 1 (PAR-1) 激动剂肽。 它对应于 PAR1 栓系配体,可以选择性地模拟凝血酶通过该受体的作用。 | |||
T39587 |
APJ receptor agonist 4
|
||
APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease. | |||
T38139 |
Orexin receptor antagonist 2
|
||
Orexin Receptor Antagonist 2 (compound 30), characterized by its potent antagonistic activity with pKis of 7.69 and 9.78, holds promise for insomnia research[1]. | |||
T40307 |
Adenosine receptor antagonist 1
|
||
Adenosine receptor antagonist 1 is a highly selective antagonist for the A2aR adenosine receptor, exhibiting an IC50 value of 0.29 nM. It demonstrates a remarkable 14-fold selectivity towards the A2aR receptor in comparison to the A2bR receptor. | |||
T37223 |
Glucagon Receptor Antagonist I
|
||
Glucagon receptor antagonist I is a competitive antagonist of the glucagon receptor (GCGR; IC50 = 181 nM). It blocks glucagon-induced glycogenolysis in primary human hepatocytes and isolated liver. Glucagon receptor antagonist I, at 50 mg/kg, reduces the increase in glucose levels observed after intraperitoneal administration of glucagon in humanized mice. Glucagon receptor antagonist inactive control does not prevent glucagon-mediated actions. | |||
T40697 |
Glucocorticoids receptor agonist 2
|
||
Glucocorticoid receptor agonist 2 is a highly effective anti-inflammatory compound, derived from arylpyrazole, that actively binds to and activates the glucocorticoid receptor. This compound exhibits potent anti-inflammatory properties without disrupting insulin secretion. | |||
T40808 |
Glucocorticoids receptor agonist 1
|
||
Glucocorticoids receptor agonist 1 (GRA-1) is a highly effective arylpyrazole-based compound that acts as an agonist for the glucocorticoid receptor. GRA-1 exhibits strong anti-inflammatory properties while maintaining insulin secretion function. | |||
T40999 | NMDA receptor antagonist 2 | ||
NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease. | |||
T40893 |
Estrogen receptor modulator 6
|
||
Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β with a remarkable affinity (K i = 0.44 nM). This compound exhibits an impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM). | |||
T39813 |
APJ receptor agonist 1
|
||
APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research. | |||
T36580 |
Glucagon Receptor Antagonist Inactive Control
|
||
Glucagon Receptor Antagonist Inactive Control 是一种 Glucagon 受体拮抗剂,可用于生命科学领域的相关研究。其产品编号为 T36580,CAS号为 362482-00-6。 | |||
T39561 |
Orexin 2 Receptor Agonist 2
|
||
Orexin 2 Receptor Agonist 2 (ORA-2) is a specific agonist for the orexin 2 receptor. | |||
T36553 |
Thrombin Receptor Peptide Ligand (trifluoroacetate salt)
|
||
Thrombin receptor peptide ligand is antagonist of the thrombin receptor (EC50s = 16-33 μM to inhibit platelet aggregation in vitro). It inhibits α-thrombin and platelet aggregation induced by thrombin receptor activating peptide in vitro when used at a concentration of 32 μM but does not affect platelet aggregation induced by ADP or collagen. It also inhibits thrombin- and TRAP-induced proliferation of vascular smooth muscle cells (VSMCs). Thrombin receptor peptide ligand (100 μmol/kg bolus, i.v... | |||
T36777 |
Thrombin Receptor Agonist Peptide (trifluoroacetate salt)
|
||
Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α... | |||
T40234 | Ghrelin receptor full agonist-2 | ||
Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S0581 |
Sec-O-Glucosylhamaudol
亥茅酚苷,Hamaudol 3-glucoside |
Others; Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others |
Sec-O-Glucosylhamaudol (Hamaudol 3-glucoside) 是从滨海前胡中分离得到的一种天然产物,能够降低 μ 阿片受体的蛋白水平,可用于缓解疼痛的研究。它通过调节脂多糖刺激的 RAW264.7 细胞系中的 p38 丝裂原活化蛋白激酶具有抗炎作用。 | |||
T5S2360 |
Corydaline
Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline |
P450; Virus Protease; Opioid Receptor; AChE | Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience |
Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱,是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运,促进胃的调节,具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。 | |||
T83913 |
Mitraciliatine
|
||
Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。 |