Adenosine Receptor
抑制剂选择性比较
Adenosine Receptor产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6619New |
ABT 702 dihydrochlorideABT-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。 |
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| S8314 |
5-Iodotubercidin5-Iodotubercidin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。 |
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| S2790 |
IstradefyllineIstradefylline是腺苷A2A受体(A2AR)选择性拮抗剂，Ki为2.2 nM。Phase 3。 |
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) |
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| S8575 |
A2AR antagonist 1A2AR 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。 |
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| S6639New |
BAY-545BAY-545是一种A2B adenosine receptor拮抗剂，ic50为59 nM。 |
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| S6646New |
CPI-444CPI-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。 |
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| S4932 |
ProxyphyllineProxyphylline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。 |
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| S8105 |
ZM241385ZM-241385是一种高亲和力的腺苷A2A受体拮抗剂。 |
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.
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| S8104 |
SCH58261SCH 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Ki值分别为2.3 nM和2 nM。 |
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| S7588 |
ReversineReversine是一种强效human A3 adenosine receptor拮抗剂，Ki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。 |
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. |
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| S8720 |
AZD-4635 (HTL1071)AZD-4635 (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。 |
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| S5427 |
AlloxazineAlloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor. |
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| S3988 |
Theophylline-7-acetic acidTheophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. |
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| S2153 |
CGS 21680 HClCGS 21680 HCl是一种adenosine A2 receptor激动剂，Ki为27 nM，比作用于A1受体选择性高140倍。 |
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.
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| S1647 |
AdenosineAdenosine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。 |
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| S5358 |
RegadenosonRegadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6619New |
ABT 702 dihydrochlorideABT-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。 |
||
| S8314 |
5-Iodotubercidin5-Iodotubercidin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。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2790 |
IstradefyllineIstradefylline是腺苷A2A受体(A2AR)选择性拮抗剂，Ki为2.2 nM。Phase 3。 |
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) |
|
| S8575 |
A2AR antagonist 1A2AR 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。 |
||
| S6639New |
BAY-545BAY-545是一种A2B adenosine receptor拮抗剂，ic50为59 nM。 |
||
| S6646New |
CPI-444CPI-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。 |
||
| S4932 |
ProxyphyllineProxyphylline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。 |
||
| S8105 |
ZM241385ZM-241385是一种高亲和力的腺苷A2A受体拮抗剂。 |
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.
|
|
| S8104 |
SCH58261SCH 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Ki值分别为2.3 nM和2 nM。 |
||
| S7588 |
ReversineReversine是一种强效human A3 adenosine receptor拮抗剂，Ki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。 |
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 |
AZD-4635 (HTL1071)AZD-4635 (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 |
AlloxazineAlloxazine 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 acidTheophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2153 |
CGS 21680 HClCGS 21680 HCl是一种adenosine A2 receptor激动剂，Ki为27 nM，比作用于A1受体选择性高140倍。 |
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 |
AdenosineAdenosine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。 |
||
| S5358 |
RegadenosonRegadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity. |
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