Retinoid Receptor
抑制剂选择性比较
特异性亚型抑制剂
Retinoid Receptor产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6691New |
AGN 193109AGN 193109 is a novel class of RAR antagonists which effectively block hormoneinduced activation and is the most potent and effective antagonist of RARα, RARβ, and RARγ, with Kd values of 2 nM, 2 nM, and 3 nM, respectively. |
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| S1653 |
TretinoinTretinoin，是 Retinoic acid receptor (RAR) 和Retinoid X receptor (RXR)的配体，作用于急性早幼粒细胞白血病（APL）细胞，诱导粒细胞分化和凋亡。 |
HL60 differentiation measured by expression of CD11b (flow cytometry) after a single dose exposure to HH1 or MC180295 for 4 days. 1 mM ATRA and high concentrations of DMSO (1.25%) were used as positive controls.
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| S2098 |
BexaroteneBexarotene 是一种维甲酸，特定选择性作用于维甲酸X受体，用作口服的抗肿瘤药，治疗皮肤T细胞淋巴瘤。 |
Bexarotene inhibited microglia activation after SAH. Left, Representative immunofluorescent images of Iba1 (red) and DAPI (blue) in basal cortex at 24 h after SAH (N = 4/group, mean ± SD). Scale bar, 30 μm. Right, quantification of Iba1 positive cells per mm2. ***p < 0.001 compared with the Sham group, ###p < 0.001 compared with the SAH + vehicle group.
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| S1276 |
AdapaleneAdapalene是一类RAR和RXR双重的激动剂，主要用于治疗痤疮。 |
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| S1368 |
AcitretinAcitretin 是一种二代维甲酸，用于治疗牛皮癣。 |
Acitretin does not induce HIV reactivation in J-lat and ACH-2 cells. (a, b) HIV reactivation induced by acid retinoic (AR) derivative acitretin (25 – 1 μM) in J-Lat cells clone 8.4 (a) and 9.2(b). HDAC inhibitors (HDCAi) panobinostat (PNB, 0.16μM) and vorinostat (VOR, 4 – 0.16 μM) were used as controls. Reactivation was determined by the quantification of GFP+ cells (%) after culturing J-Lat with HDACi and acitretin for 24h. (c, d) HIV reactivation induced by acitretin and HDACi in ACH-2 cells. Reactivation was determined after 48h of incubation by quantification of CAp24 (c) and HIV RNA copy number (d) in the supernatant. Values represent mean±SD of at least three independent experiments performed in triplicate. UN, untreated. *P < 0.05; **P < 0.01; ***P < 0.001.
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| S1569 |
TazaroteneTazarotene是RAR激动剂tazarotenic acid的前药，用于治疗牛皮癣，粉刺以及晒伤。 |
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| S2933New |
AM580AM580是视黄酸核受体（RAR）激动剂，对RARα, RARβ和RARγ的Kd值分别为8 nM, 131 nM 和450 nM。 |
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| S6132New |
All trans-RetinalAll trans-Retinal是维甲酸循环中的组分之一，在体内通过视黄醛脱氢酶转化为视黄酸。Retinoic acid是RAR和RXR的配体。All trans-retinal是一种有效的光敏剂。 |
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| S4627 |
TTNPB (Arotinoid Acid)TTNPB (Arotinoid Acid)是有效的RAR激动剂, 抑制与[3H]tRA结合,作用于人类RARα, β, 和 γ, IC50分别为5.1 nM, 4.5 nM,和 9.3 nM。 |
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| S4260 |
TamibaroteneTamibarotene是特异性的RAR-alpha/beta激动剂, 用于治疗全反式视黄酸耐受的急性白血病。 |
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| S4699 |
EtretinateEtretinate是可口服的芳香类维生素a酸，在牛皮鲜和其他皮肤综合症的治疗中十分有效。它能够激活视黄素受体，诱导细胞分化、抑制细胞增殖以及抑制组织浸润。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6691New |
AGN 193109AGN 193109 is a novel class of RAR antagonists which effectively block hormoneinduced activation and is the most potent and effective antagonist of RARα, RARβ, and RARγ, with Kd values of 2 nM, 2 nM, and 3 nM, respectively. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1653 |
TretinoinTretinoin，是 Retinoic acid receptor (RAR) 和Retinoid X receptor (RXR)的配体，作用于急性早幼粒细胞白血病（APL）细胞，诱导粒细胞分化和凋亡。 |
HL60 differentiation measured by expression of CD11b (flow cytometry) after a single dose exposure to HH1 or MC180295 for 4 days. 1 mM ATRA and high concentrations of DMSO (1.25%) were used as positive controls.
|
|
| S2098 |
BexaroteneBexarotene 是一种维甲酸，特定选择性作用于维甲酸X受体，用作口服的抗肿瘤药，治疗皮肤T细胞淋巴瘤。 |
Bexarotene inhibited microglia activation after SAH. Left, Representative immunofluorescent images of Iba1 (red) and DAPI (blue) in basal cortex at 24 h after SAH (N = 4/group, mean ± SD). Scale bar, 30 μm. Right, quantification of Iba1 positive cells per mm2. ***p < 0.001 compared with the Sham group, ###p < 0.001 compared with the SAH + vehicle group.
|
|
| S1276 |
AdapaleneAdapalene是一类RAR和RXR双重的激动剂，主要用于治疗痤疮。 |
||
| S1368 |
AcitretinAcitretin 是一种二代维甲酸，用于治疗牛皮癣。 |
Acitretin does not induce HIV reactivation in J-lat and ACH-2 cells. (a, b) HIV reactivation induced by acid retinoic (AR) derivative acitretin (25 – 1 μM) in J-Lat cells clone 8.4 (a) and 9.2(b). HDAC inhibitors (HDCAi) panobinostat (PNB, 0.16μM) and vorinostat (VOR, 4 – 0.16 μM) were used as controls. Reactivation was determined by the quantification of GFP+ cells (%) after culturing J-Lat with HDACi and acitretin for 24h. (c, d) HIV reactivation induced by acitretin and HDACi in ACH-2 cells. Reactivation was determined after 48h of incubation by quantification of CAp24 (c) and HIV RNA copy number (d) in the supernatant. Values represent mean±SD of at least three independent experiments performed in triplicate. UN, untreated. *P < 0.05; **P < 0.01; ***P < 0.001.
|
|
| S1569 |
TazaroteneTazarotene是RAR激动剂tazarotenic acid的前药，用于治疗牛皮癣，粉刺以及晒伤。 |
||
| S2933New |
AM580AM580是视黄酸核受体（RAR）激动剂，对RARα, RARβ和RARγ的Kd值分别为8 nM, 131 nM 和450 nM。 |
||
| S6132New |
All trans-RetinalAll trans-Retinal是维甲酸循环中的组分之一，在体内通过视黄醛脱氢酶转化为视黄酸。Retinoic acid是RAR和RXR的配体。All trans-retinal是一种有效的光敏剂。 |
||
| S4627 |
TTNPB (Arotinoid Acid)TTNPB (Arotinoid Acid)是有效的RAR激动剂, 抑制与[3H]tRA结合,作用于人类RARα, β, 和 γ, IC50分别为5.1 nM, 4.5 nM,和 9.3 nM。 |
||
| S4260 |
TamibaroteneTamibarotene是特异性的RAR-alpha/beta激动剂, 用于治疗全反式视黄酸耐受的急性白血病。 |
||
| S4699 |
EtretinateEtretinate是可口服的芳香类维生素a酸，在牛皮鲜和其他皮肤综合症的治疗中十分有效。它能够激活视黄素受体，诱导细胞分化、抑制细胞增殖以及抑制组织浸润。 |
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