Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10305 |
Amiselimod hydrochloride
MT-1303 hydrochloride |
S1P Receptor; LPL Receptor | GPCR/G Protein |
Amiselimod hydrochloride (MT-1303 hydrochloride) 是一种鞘氨醇 1-磷酸受体 1 (S1P1) 调节剂。 | |||
T14301 |
Apararenone
MT-3995 |
Glucocorticoid Receptor | Endocrinology/Hormones |
Apararenone (MT-3995) 是一种新型的、非甾体类盐皮质激素受体 (mineralocorticoid receptor) 拮抗剂,正在开发用于糖尿病性肾病和非酒精性脂肪性肝炎的研究。 | |||
T15034 |
Roluperidone
CYR-101,MIN-101,MT-210 |
Sigma receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Roluperidone (CYR-101) 是一种新型环酰胺衍生物,对5-HT2A 和sigma-2受体具有高亲和力,Ki 分别为 7.53 和 8.19 nM。 | |||
T6973 |
RS-127445
MT500 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
RS-127445 (MT500) 是一种可口服的高亲和力选择性5-HT2B 受体拮抗剂,pKi 为 9.5,pIC50 为 10.4,比作用于其他受体和离子通道的选择性高 1000 倍。 | |||
T7519 |
RS-127445 hydrochloride
4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐,RS 127445,MT 500 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
RS-127445 hydrochloride (MT 500) 是一种可口服的,高亲和力选择性5-HT2B 受体拮抗剂,pKi 为 9.5,比作用于其他受体和离子通道的选择性高 1000 倍。 | |||
TP1097 |
Melanotan I
美拉诺坦,美拉诺坦 I,[Nle4,D-Phe7]-α-MSH,Afamelanotide,MT-I |
Others | Others |
Melanotan I 是一种非特异性黑素皮质激素受体 (MCR) 激动剂, 是一种 α- 黑素细胞刺激激素 (α-MSH) 类似物,皮下注射可增加黑色素在皮肤中的含量。Melanotan I 可用于辅助美黑。Melanotan I 可用于预防阳光诱发皮肤癌,可用于研究黑色素瘤和男性勃起功能障碍。 | |||
T7589 |
Afamelanotide acetate
afamelanotide |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Afamelanotide acetate 是一种合成的 α-黑素细胞刺激激素类似物和一流的黑皮质素-1 受体激动剂,用于治疗红细胞生成性原卟啉症。 | |||
T1900 |
LDN-212854
LDN212854,BMP Inhibitor III |
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
LDN-212854 (BMP Inhibitor III) 是一种新型BMP 抑制剂,抑制 ALK2 的IC50=1.3 nM,比对ALK1,ALK3,ALK4和ALK5的抑制性高2,66,1641和7135倍。 | |||
TP1324 |
Melanotan (MT)-II
美拉诺坦 II,美拉诺坦 (MT)-II |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Melanotan (MT)-II 是一种可注射用的多肽荷尔蒙,是合成的黑皮质素受体激动剂,能够促进晒黑。 | |||
T25310 |
Dersimelagon
MT-7117 |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Dersimelagon (MT-7117) (MT-7117) 是一种具有口服活性的选择性黑皮质素 1 受体(MC1R) 激动剂,对人 (h)、食蟹猴 (cm)、小鼠 (m) 和大鼠 (r) MC1R 的 EC50 值分别为 8.16、3.91、1.14 和 0.251 nM。Dersimelagon 对 hMC1R 和 hMC4R 表现出良好的亲和力,Ki 值分别为 2.26 和 32.9 nM。Dersimelagon 可用于皮肤色素沉着的研究。 | |||
T1463 |
Ramelteon
雷美替胺,TAK-375 |
Melatonin Receptor; MT Receptor | GPCR/G Protein; Neuroscience |
Ramelteon (TAK-375) 是强效高选择性和可口服的 MT1/MT2激动剂,Ki 值分别为 14 和 112 pM,有用于失眠症的研究潜力。 | |||
T60490 |
Melatonin receptor agonist 1
|
||
Melatonin receptor agonist 1 (compound 20c) 是褪黑激素受体 (MT) 的有效激动剂,对MT2的Ki 值为 108 nM,对MT1的Ki 值为 1140 nM。 | |||
T29044 |
UCM 765
UCM-765,UCM765 |
||
UCM 765 is a partial agonist of melatonin MT(2) receptor. | |||
T71214 |
MT-7716 HCl hydrate
|
||
MT-7716 HCl hydrate is a NOP receptor agonist. | |||
T12120 |
MT-7716 hydrochloride
W-212393 hydrochloride |
Others | Others |
MT-7716 hydrochloride is a selective agonist of non-peptide nociceptin receptor (NOP) | |||
T12120L |
MT-7716 free base
W-212393 |
Others | Others |
MT-7716 free base is a selective non-peptide agonist of nociceptin receptor (NOP). It is used for promising potential treatment drugs for alcohol abuse and relapse prevention. | |||
T70035 |
Tasimelteon-d5
|
||
Tasimelteon-d5 is intended for use as an internal standard for the quantification of tasimelteon by GC- or LC-MS. Tasimelteon is a melatonin (MT) receptor agonist. It selectively binds MT1 and MT2 receptors over a panel of 160 additional receptors and enzymes at 10 µM. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of no... | |||
T69081 | KRH-1636 | ||
KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chem... | |||
T83769 |
TC 14012 hydrochloride
H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2 |
||
TC 14012是一种化学肽模拟的拮抗剂,针对趋化因子(C-X-C motif)受体4(CXCR4;IC50 = 2.9 nM)和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募(EC50 = 350 nM)。TC 14012可减少HIV在MT-4细胞中的细胞病理效应(EC50 = 0.4 nM),并以CXCR4依赖的方式抑制HIV在体外进入(IC50 = 19.3 nM)。它还能抑制由趋化因子(C-X-C motif)配体12(CXCL12)在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞(HUVECs)中诱导的迁移,当使用浓度范围从10到1,000 nM时。在通过左前降(LAD)冠状动脉结扎诱导的急性心肌梗死小鼠模型中,TC 14012(10 mg/kg)能减少梗死面积。 |