目录号 | 产品详情 | 靶点 | |
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T60047L | Glucagon Receptor | ||
V-0219 hydrochloride 是一种具有口服活性的 glucagon-like peptide-1 receptor (GLP-1R) 正向别构调节剂 (PAM)。V-0219 能被用于肥胖相关糖尿病的研究。 | |||
T8224 | AChR | ||
VU0119498 是泛 GqmAChR M1、M3和M5的正变构调节剂,具有抗糖尿病活性,EC50值分别为 6.04、6.38 和 4.08 µM。 | |||
T6727 | GluR | ||
VU0364770 (VU 0364770) 是一种选择性mGlu4正变构调节剂,对 mGlu5 具有拮抗活性,对 mGlu6 具有正变构调节活性。它还对 MAO 具有活性,对人 MAO-A 和 MAO-B 的 Ki 值分别为8.5 和 0.72 μM。 | |||
T8963 | Neuropeptide Y Receptor | ||
CYM2503 是 GAL2 受体的正变构调节剂 (PAM),可在体外增强甘丙肽诱导的 IP1 产生。它对受体的正构甘丙肽结合位点没有亲和力(通过其无法置换碘化甘丙肽或自行诱导 IP1 积累来衡量)。 | |||
T8741 | Others | ||
MitoBloCK-10 (3-fluoro-N'-[(E)-(5-nitrothiophen-2-yl)m) 是第一个能够减弱PAM 复合体活性的小分子调节剂,对 C 末端结构域的Tim44与前体和 Hsp70 结合具有抑制作用。 | |||
T67729 | Dopamine Receptor | ||
UCM-1306 是具有口服活性的人多巴胺 D1 受体变构调节剂 (PAM)。UCM-1306 增加结合在人和小鼠 D1 受体的内源性多巴胺 (DA) 效应。UCM-1306可以改善运动症状,解决与长期帕金森病(PD) 相关的关键共病认知障碍。 | |||
T23440 | GluR | ||
TC-N 22A 是一种作用力强的、可选择的、口服具有活性的、可以通过血脑屏障的 mGlu4 正向别构调节剂 (PAM)。TC-N 22A 在表达人 mGlu4 的 BHK 细胞中 EC50 表现为 9 nM。TC-N 22A 在激动和正向别构模型中对 mGlu 1、2、3、5 和 7 受体的活性表现很低 (EC50 >10 μM)。TC-N 22A 可以用于中枢神经系统疾病的研究。 | |||
T35028 | GluR | ||
Valiglurax (VU2957),也称为 VU0652957和 VU2957,是一种强效、选择性、中枢神经系统渗透剂,可口服生物利用的 mGlu4正变构调节剂。VU2957具有良好的跨物种的体内外药理学和药代动力学性质。VU2957被评估为治疗帕金森病的临床前开发候选药物。 | |||
T6726 | GluR | ||
VU0361737 (ML-128) 是一种高效选择性的,中枢神经系统渗透性的代谢型谷氨酸受体 4(mGluR4)正变构调节剂,对人类和大鼠 mGluR4作用的EC50值分别为 240 和 110 nM。它具有神经保护作用,有用于帕金森氏病的研究潜力。 | |||
T2067 | GABA Receptor | ||
NS11394 是可口服GABAA 的阳性变构调节剂 (PAM),Ki 值为 0.5 nM。它对GABAA 的选择性依次为 α5、α3、α2 和α1 受体,具有抗炎和抗焦虑活性。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-00392 | PAM Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
PAM Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 94.4 kDa and the accession number is P19021-2.
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TMPY-00149 | PAM Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
PAM Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 104 kDa and the accession number is P19021-2.
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TMPK-00188 | JAM-A Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
junctional adhesion molecule A (JAM-A), a cell adhesion molecule, is highly elevated in human GBM cancer stem cells and predicts poor patient prognosis. While JAM-A is also highly expressed in other cells in the tumor microenvironment, specifically microglia and macrophages,JAM-A functions to suppress pathogenic microglial activation in the female tumor microenvironment, highlighting an emerging role for sex differences in the GBM microenvironment and suggesting that sex differences extend beyond previously reported tumor cell-intrinsic differences.
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TMPY-01035 | JAM-A Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
JAM-A Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 25 kDa and the accession number is Q9Y624-1.
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TMPY-00865 | JAM-A Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
JAM-A Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 50 kDa and the accession number is Q9BQB4-1.
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TMPJ-00965 | TIM16 Protein, S. cerevisiae, Recombinant | S. cerevisiae | E. coli | ||
Mitochondrial import inner membrane translocase subunit TIM16 (TIM16) is an ssential component of the PAM complex. PAM complex is required for the translocation of transit peptide-containing proteins from the inner membrane into the mitochondrial matrix in an ATP-dependent manner. In the complex, TIM16 is required to regulate activity of mtHSP70 (SSC1) via its interaction with PAM18/TIM14. TIM16 may act by positioning PAM18/TIM14 in juxtaposition to mtHSP70 at the translocon to maximize ATPase stimulation.
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TMPJ-01087 | TIM14 Protein, S. cerevisiae, Recombinant | S. cerevisiae | E. coli | ||
Mitochondrial import inner membrane translocase subunit TIM14 (TIM14) is an essential component of the PAM complex. PAM complex is required for the translocation of transit peptide-containing proteins from the inner membrane into the mitochondrial matrix in an ATP-dependent manner. In the complex, TIM14 is required to stimulate activity of mtHSP70 (SSC1). TIM14 belongs to the DnaJ family, which has been involved in Hsp40/Hsp70 chaperone systems. As a mitochondrial chaperone, TIM14 functions as part of the TIM23 complex import motor to facilitate the import of nuclear-encoded proteins into the mitochondria. TIM14 also complexes with prohibitin complexes to regulate mitochondrial morphogenesis, and has been implicated in dilated cardiomyopathy with ataxia.
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TMPH-01690 | TIM14 Protein, Human, Recombinant (GST) | Human | E. coli | ||
Mitochondrial co-chaperone which forms a complex with prohibitins to regulate cardiolipin remodeling. May be a component of the PAM complex, a complex required for the translocation of transit peptide-containing proteins from the inner membrane into the mitochondrial matrix in an ATP-dependent manner. May act as a co-chaperone that stimulate the ATP-dependent activity.
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