cAMP
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
cAMP产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8414 |
PACAP 1-27垂体腺苷环化酶激活肽(PACAP 1-27)是有效的PACAP受体拮抗剂。 |
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| S7499 |
ESI-09ESI-09是一种特定的exchange protein directly activated by cAMP (EPAC)抑制剂，其对EPAC1和EPAC2的IC50分别为3.2 μM 和1.4 μM ，比PKA高出100多倍的选择性。 |
PKA but not Epac blockade reversed the JWH133-mediated effects on the microglial phenotypic conversion. PKA (H89) or Epac (ESI-09) specific inhibitors were treated with JWH133. qPCR was used to investigate mRNA expression of the M1 markers CD86 (A) and CD68 (B), as well as the M2 markers Ym1 (D) and CD206 (E). Western blot analysis was conducted, and the relative CD68 (C) and CD206 (F) densities were evaluated for further determinations. The data are expressed as means ± SD. **P < 0.01, ***P < 0.001 vs. Throm; #P < 0.05, ##P < 0.01 vs. Throm + JWH; n = 3 per group. |
|
| S8416 |
PACAP 6-38PACAP 6-38 是PACAP (pituitary adenylate cyclase-activating polypeptide)的非刺激性竞争性拮抗剂，IC50为2 nM。在体内，它还能作为功能性的CARTp拮抗剂。 |
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| S6850New |
NE 52-QQ57NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂，其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累，在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加，包括 tumor necrosis factor-α (TNF-α)、interleukin (IL)-1β、IL-6、inducible nitric oxide synthase (iNOS)、nitric oxide (NO)、cyclooxygenase 2 (COX2) 和 prostaglandin E2 (PGE2)。 |
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| S0451New |
ST034307ST034307 is a potent and selective inhibitor of adenylyl cyclase 1 (AC1) with IC50 of 2.3 μM. |
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| S7500 |
HJC0350HJC0350 是强效的选择性的EPAC2抑制剂，IC50为0.3 μM,对Epac1无抑制作用。 |
||
| S8283 |
SQ22536SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine)是腺苷酸环化酶的抑制剂。可在完整人类血小板中抑制PGE-1刺激的cAMP水平升高。 |
Effects of AC inhibitor SQ22536 on A20 cell proliferation and expression of cAMP, Reelin, CDK5, IL-10 and caspase-3. (A) The expression level of cAMP in A20 cells treated with SQ22536 using ELISA assay. (B) The proliferation rate analysis of A20 cell treated with SQ22536 using CCK-8 assay. (C) Western blotting determined the expression levels of Reelin, CDK5, caspase-3 and IL-10 in A20 treated with SQ22536. **p<0.01.
|
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| S6478 |
Fipexide hydrochlorideFipexide (hydrochloride)是哌嗪类的精神药物。 |
||
| S4552 |
BithionolBithionol (Actamer)是有效的sAC（可溶性腺苷酸环化酶）抑制剂，IC50为4 μM。具有抗菌、驱肠虫以及除海藻活性。 |
||
| S2449 |
Colforsin (Forskolin)Colforsin (Forskolin, Coleonol, Colforsin) 在各种各样细胞类型中，是一种普遍存在的真核细胞腺苷酸环化酶（AC）激活剂，在细胞生理学研究中，通常用来提高cAMP水平。Forskolin 还可激发 PXR 和 FXR的活性而诱导自噬。 |
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| S8415 |
PACAP 1-38PACAP 1-38 (Pituitary Adenylate Cyclase Activating Polypeptide 38)是高度有效的PACAP受体激动剂（Kd=100 pM），能够刺激腺苷酸环化酶和吞噬作用。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8414 |
PACAP 1-27垂体腺苷环化酶激活肽(PACAP 1-27)是有效的PACAP受体拮抗剂。 |
||
| S7499 |
ESI-09ESI-09是一种特定的exchange protein directly activated by cAMP (EPAC)抑制剂，其对EPAC1和EPAC2的IC50分别为3.2 μM 和1.4 μM ，比PKA高出100多倍的选择性。 |
PKA but not Epac blockade reversed the JWH133-mediated effects on the microglial phenotypic conversion. PKA (H89) or Epac (ESI-09) specific inhibitors were treated with JWH133. qPCR was used to investigate mRNA expression of the M1 markers CD86 (A) and CD68 (B), as well as the M2 markers Ym1 (D) and CD206 (E). Western blot analysis was conducted, and the relative CD68 (C) and CD206 (F) densities were evaluated for further determinations. The data are expressed as means ± SD. **P < 0.01, ***P < 0.001 vs. Throm; #P < 0.05, ##P < 0.01 vs. Throm + JWH; n = 3 per group. |
|
| S8416 |
PACAP 6-38PACAP 6-38 是PACAP (pituitary adenylate cyclase-activating polypeptide)的非刺激性竞争性拮抗剂，IC50为2 nM。在体内，它还能作为功能性的CARTp拮抗剂。 |
||
| S6850New |
NE 52-QQ57NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂，其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累，在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加，包括 tumor necrosis factor-α (TNF-α)、interleukin (IL)-1β、IL-6、inducible nitric oxide synthase (iNOS)、nitric oxide (NO)、cyclooxygenase 2 (COX2) 和 prostaglandin E2 (PGE2)。 |
||
| S0451New |
ST034307ST034307 is a potent and selective inhibitor of adenylyl cyclase 1 (AC1) with IC50 of 2.3 μM. |
||
| S7500 |
HJC0350HJC0350 是强效的选择性的EPAC2抑制剂，IC50为0.3 μM,对Epac1无抑制作用。 |
||
| S8283 |
SQ22536SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine)是腺苷酸环化酶的抑制剂。可在完整人类血小板中抑制PGE-1刺激的cAMP水平升高。 |
Effects of AC inhibitor SQ22536 on A20 cell proliferation and expression of cAMP, Reelin, CDK5, IL-10 and caspase-3. (A) The expression level of cAMP in A20 cells treated with SQ22536 using ELISA assay. (B) The proliferation rate analysis of A20 cell treated with SQ22536 using CCK-8 assay. (C) Western blotting determined the expression levels of Reelin, CDK5, caspase-3 and IL-10 in A20 treated with SQ22536. **p<0.01.
|
|
| S6478 |
Fipexide hydrochlorideFipexide (hydrochloride)是哌嗪类的精神药物。 |
||
| S4552 |
BithionolBithionol (Actamer)是有效的sAC（可溶性腺苷酸环化酶）抑制剂，IC50为4 μM。具有抗菌、驱肠虫以及除海藻活性。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2449 |
Colforsin (Forskolin)Colforsin (Forskolin, Coleonol, Colforsin) 在各种各样细胞类型中，是一种普遍存在的真核细胞腺苷酸环化酶（AC）激活剂，在细胞生理学研究中，通常用来提高cAMP水平。Forskolin 还可激发 PXR 和 FXR的活性而诱导自噬。 |
|
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8415 |
PACAP 1-38PACAP 1-38 (Pituitary Adenylate Cyclase Activating Polypeptide 38)是高度有效的PACAP受体激动剂（Kd=100 pM），能够刺激腺苷酸环化酶和吞噬作用。 |
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