Adenosine Receptor

抑制剂选择性比较

Adenosine Receptor产品

所有产品(21) Adenosine Receptor抑制剂(3) Adenosine Receptor拮抗剂(12) Adenosine Receptor激动剂(6)

目录号	产品描述	文献引用	实验数据
S0721^New	Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) 是一种 adenosine diphosphate (ADP) 诱导的 platelet aggregation 的口服活性抑制剂。Ticlopidine 也是 CYP2B6 的抑制剂，Ki值为0.2 μM。
S8314	5-Iodotubercidin 5-Iodotubercidin (NSC 113939, 5-ITu) 是有效的腺苷激酶抑制剂，IC50为26 nM。它可抑制核苷转运蛋白、CK1、胰岛素受体酪氨酸激酶、PKA、CK2和PKC。	Oncogene, 2020, 16
S6619	ABT 702 dihydrochloride ABT-702是一种新型的、有效的非核苷类Adenosine kinase（腺苷激酶）抑制剂，IC50为0.7 nM。它在动物炎症和疼痛模型中具有口服活性。
S2790	Istradefylline Istradefylline (KW-6002) 是腺苷A2A受体(A2AR)选择性拮抗剂，K_i为2.2 nM。Phase 3。	Cell Metab, 2018, 28(3):476-489 Neurotox Res, 2015, 27(3):229-45	The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)
S6910^New	Preladenant Preladenant (Privadenant, SCH 420814, MK-3814) 是一种有效的人类 adenosine A_2A receptor 的竞争性的、选择性的拮抗剂，Ki值为1.1 nM。
S8575	A2AR antagonist 1 A2AR antagonist 1是有效的A2AR (Adenosine A2A Receptor)拮抗剂，对A2AR和A1R的Ki值分别为4 nM和264 nM。	Mol Cancer Res, 2019, 17(5):1166-1179
S4932	Proxyphylline Proxyphylline (Monophylline, Spasmolysin) 是茶碱（theophylline）的衍生物，被用作支气管扩张剂。它能够选择性地拮抗A1 adenosine receptors。
S6646	CPI-444 CPI-444是一种有效的选择性Adenosine A2A receptor拮抗剂，它与A2AR结合，Ki值为3.54 nM，对A2AR的选择性比对其他腺苷受体亚型高50倍以上。
S8105	ZM241385 ZM-241385是一种高亲和力的腺苷A2A受体拮抗剂。	Cell Mol Immunol, 2020, 10 Biomed Res Int, 2020, 2020:2603873 Oxid Med Cell Longev, 2020, 2020:7649080	T cells treated with MTX, astilbin, ZM241385 and SCH772984. The levels of p-ERK1/2, p-P65, p-STAT1 and p-STAT3 were analyzed by western blot.
S6639	BAY-545 BAY-545是一种A_2B adenosine receptor拮抗剂，ic50为59 nM。
S8104	SCH58261 SCH 58261是一个高效的选择性的A2a adenosine receptor拮抗剂，其对rat A2a和bovine A2a的K_i值分别为2.3 nM和2 nM。	Haematologica, 2020, 16 pii: haematol PPAR Res, 2020, 2020:2410264 J Neurochem, 2020, 10.1111/jnc.15146
S7588	Reversine Reversine是一种强效human A3 adenosine receptor拮抗剂，K_i为0.66 μM，也是一种泛aurora A/B/C kinase抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞分化。	Nat Methods, 2020, 17(3):279-282 J Cell Physiol, 2020, 235(3):2441-2451 Nat Commun, 2019, 10(1):4224	Immunofluorescence of acetylated a-tubulin (red) in control (a), reversin-treated (b), and BI 2536/Reversin mixture-treated embryos (c).The embryos treated with Reversine completed first mitosis, but the nuclei of their blastomeres were fragmented (b, arrows). Embryos inhibited withthe BI 2536/Reversine mixture arrested before the onset of anaphase. Microtubules of the spindle are disorganized (c, double-arrow) and thechromosomes are misaligned (c, arrows) in these inhibited embryos. DNA is counter-stained with DAPI (blue). Scale bar, 10 μm.
S8720	AZD4635 (HTL1071) AZD4635 (HTL1071)是一种口服的A2AR拮抗剂，可与人源A2AR结合，Ki值为1.7 nM，对A2AR的选择性是对其他腺苷受体的30倍以上。
S5427	Alloxazine Alloxazine (Isoalloxazine) is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.
S3988	Theophylline-7-acetic acid Theophylline-7-acetic acid (Acefylline, acetyloxytheophylline, Carboxymethyltheophylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.
S2153	CGS 21680 HCl CGS 21680 HCl是一种adenosine A2 receptor激动剂，K_i为27 nM，比作用于A1受体选择性高140倍。	Biomed Res Int, 2020, 2020:2603873 PPAR Res, 2020, 2020:2410264 J Neurochem, 2020, 10.1111/jnc.15146	Effects of CGS-21,680 and forskolin on caffeine inhibited the expression of leptin in the human BeWo cells. The cells were treated with CGS-21,680 (2 μM, adenosine receptor A2a (ADORA2A) agonist)/forskolin (4 μM, adenylyl cyclase (AC) agonist, cAMP activator) and/or caffeine (20 μM) for 7 d. (A and B) The mRNA expression of leptin and ADORA2A was detected by quantitative real-time PCR, n = 3. (C) The protein expression of ADORA2A was detected by Western blotting, n = 2. (D) At the end of the treatment, the mRNA expression of leptin was detected by real-time PCR, n = 3. GAPDH was used as an internal control. The results are expressed as the mean ± S.E.M. of three independent experiments; P < 0.05 and *P < 0.01 vs. control.
S1647	Adenosine Adenosine是一种核苷，包含腺嘌呤，通过β-N9-糖苷键，与核糖分子（呋喃核糖的）部分连接。	Front Cell Neurosci, 2018, 12:139 ACS Appl Mater Interfaces, 2016, 8(39):25818-25824 Biogerontology, 2016, 17(5-6):907-920
S5358	Regadenoson Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
S0498^New	Namodenoson (CF-102) Namodenoson (CF-102, 2-Cl-IB-MECA) 是一种口服生物利用的 A3 adenosine receptor (A3AR) 的选择性激动剂，Ki值为0.33 nM。Namodenoson 具有使PI3K/NF‑κB/Wnt/β‑catenin信号通路失调来介导的抗NASH作用。
S9608^New	AB928 AB928 (A2aR/A2bR antagonist-1)是一种新型的 A2aR/A2bR 的双重活性拮抗剂，对于A2aR和A2bR的Kd值分别为1.4 nM和2 nM。
S5678	trans-Zeatin-riboside Zeatin Riboside is the most active and ubiquitous form of the naturally occurring cytokinins that promote cell division, stimulate shoot proliferation, inhibit root formation, slow the aging process, and activate gene expression and metabolic activity.

目录号

产品描述

文献引用

实验数据

S0721^New

Ticlopidine

Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) 是一种 adenosine diphosphate (ADP) 诱导的 platelet aggregation 的口服活性抑制剂。Ticlopidine 也是 CYP2B6 的抑制剂，Ki值为0.2 μM。

S8314

5-Iodotubercidin

5-Iodotubercidin (NSC 113939, 5-ITu) 是有效的腺苷激酶抑制剂，IC50为26 nM。它可抑制核苷转运蛋白、CK1、胰岛素受体酪氨酸激酶、PKA、CK2和PKC。

Oncogene,2020, 16

S6619

ABT 702 dihydrochloride

ABT-702是一种新型的、有效的非核苷类Adenosine kinase（腺苷激酶）抑制剂，IC50为0.7 nM。它在动物炎症和疼痛模型中具有口服活性。

目录号	产品描述	文献引用	实验数据
S2790	Istradefylline Istradefylline (KW-6002) 是腺苷A2A受体(A2AR)选择性拮抗剂，K_i为2.2 nM。Phase 3。	Cell Metab, 2018, 28(3):476-489 Neurotox Res, 2015, 27(3):229-45	The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)
S6910^New	Preladenant Preladenant (Privadenant, SCH 420814, MK-3814) 是一种有效的人类 adenosine A_2A receptor 的竞争性的、选择性的拮抗剂，Ki值为1.1 nM。
S8575	A2AR antagonist 1 A2AR antagonist 1是有效的A2AR (Adenosine A2A Receptor)拮抗剂，对A2AR和A1R的Ki值分别为4 nM和264 nM。	Mol Cancer Res, 2019, 17(5):1166-1179
S4932	Proxyphylline Proxyphylline (Monophylline, Spasmolysin) 是茶碱（theophylline）的衍生物，被用作支气管扩张剂。它能够选择性地拮抗A1 adenosine receptors。
S6646	CPI-444 CPI-444是一种有效的选择性Adenosine A2A receptor拮抗剂，它与A2AR结合，Ki值为3.54 nM，对A2AR的选择性比对其他腺苷受体亚型高50倍以上。
S8105	ZM241385 ZM-241385是一种高亲和力的腺苷A2A受体拮抗剂。	Cell Mol Immunol, 2020, 10 Biomed Res Int, 2020, 2020:2603873 Oxid Med Cell Longev, 2020, 2020:7649080	T cells treated with MTX, astilbin, ZM241385 and SCH772984. The levels of p-ERK1/2, p-P65, p-STAT1 and p-STAT3 were analyzed by western blot.
S6639	BAY-545 BAY-545是一种A_2B adenosine receptor拮抗剂，ic50为59 nM。
S8104	SCH58261 SCH 58261是一个高效的选择性的A2a adenosine receptor拮抗剂，其对rat A2a和bovine A2a的K_i值分别为2.3 nM和2 nM。	Haematologica, 2020, 16 pii: haematol PPAR Res, 2020, 2020:2410264 J Neurochem, 2020, 10.1111/jnc.15146
S7588	Reversine Reversine是一种强效human A3 adenosine receptor拮抗剂，K_i为0.66 μM，也是一种泛aurora A/B/C kinase抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞分化。	Nat Methods, 2020, 17(3):279-282 J Cell Physiol, 2020, 235(3):2441-2451 Nat Commun, 2019, 10(1):4224	Immunofluorescence of acetylated a-tubulin (red) in control (a), reversin-treated (b), and BI 2536/Reversin mixture-treated embryos (c).The embryos treated with Reversine completed first mitosis, but the nuclei of their blastomeres were fragmented (b, arrows). Embryos inhibited withthe BI 2536/Reversine mixture arrested before the onset of anaphase. Microtubules of the spindle are disorganized (c, double-arrow) and thechromosomes are misaligned (c, arrows) in these inhibited embryos. DNA is counter-stained with DAPI (blue). Scale bar, 10 μm.
S8720	AZD4635 (HTL1071) AZD4635 (HTL1071)是一种口服的A2AR拮抗剂，可与人源A2AR结合，Ki值为1.7 nM，对A2AR的选择性是对其他腺苷受体的30倍以上。
S5427	Alloxazine Alloxazine (Isoalloxazine) is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.
S3988	Theophylline-7-acetic acid Theophylline-7-acetic acid (Acefylline, acetyloxytheophylline, Carboxymethyltheophylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.

目录号	产品描述	文献引用	实验数据
S2153	CGS 21680 HCl CGS 21680 HCl是一种adenosine A2 receptor激动剂，K_i为27 nM，比作用于A1受体选择性高140倍。	Biomed Res Int, 2020, 2020:2603873 PPAR Res, 2020, 2020:2410264 J Neurochem, 2020, 10.1111/jnc.15146	Effects of CGS-21,680 and forskolin on caffeine inhibited the expression of leptin in the human BeWo cells. The cells were treated with CGS-21,680 (2 μM, adenosine receptor A2a (ADORA2A) agonist)/forskolin (4 μM, adenylyl cyclase (AC) agonist, cAMP activator) and/or caffeine (20 μM) for 7 d. (A and B) The mRNA expression of leptin and ADORA2A was detected by quantitative real-time PCR, n = 3. (C) The protein expression of ADORA2A was detected by Western blotting, n = 2. (D) At the end of the treatment, the mRNA expression of leptin was detected by real-time PCR, n = 3. GAPDH was used as an internal control. The results are expressed as the mean ± S.E.M. of three independent experiments; P < 0.05 and *P < 0.01 vs. control.
S1647	Adenosine Adenosine是一种核苷，包含腺嘌呤，通过β-N9-糖苷键，与核糖分子（呋喃核糖的）部分连接。	Front Cell Neurosci, 2018, 12:139 ACS Appl Mater Interfaces, 2016, 8(39):25818-25824 Biogerontology, 2016, 17(5-6):907-920
S5358	Regadenoson Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
S0498^New	Namodenoson (CF-102) Namodenoson (CF-102, 2-Cl-IB-MECA) 是一种口服生物利用的 A3 adenosine receptor (A3AR) 的选择性激动剂，Ki值为0.33 nM。Namodenoson 具有使PI3K/NF‑κB/Wnt/β‑catenin信号通路失调来介导的抗NASH作用。
S9608^New	AB928 AB928 (A2aR/A2bR antagonist-1)是一种新型的 A2aR/A2bR 的双重活性拮抗剂，对于A2aR和A2bR的Kd值分别为1.4 nM和2 nM。
S5678	trans-Zeatin-riboside Zeatin Riboside is the most active and ubiquitous form of the naturally occurring cytokinins that promote cell division, stimulate shoot proliferation, inhibit root formation, slow the aging process, and activate gene expression and metabolic activity.

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抑制剂选择性比较

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