Retinoid Receptor
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1653 | Tretinoin | <1 mg/mL | 60 mg/mL | 6 mg/mL |
| S2098 | Bexarotene | <1 mg/mL | 8 mg/mL | <1 mg/mL |
| S1276 | Adapalene | <1 mg/mL | 8 mg/mL | <1 mg/mL |
| S1368 | Acitretin | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S1569 | Tazarotene | <1 mg/mL | 10 mg/mL | 10 mg/mL |
| S6132 | All trans-Retinal | -1 mg/mL | 56 mg/mL | -1 mg/mL |
| S4627 | TTNPB (Arotinoid Acid) | <1 mg/mL | 15 mg/mL | <1 mg/mL |
| S4260 | Tamibarotene | <1 mg/mL | 70 mg/mL | 70 mg/mL |
| S4699 | Etretinate | <1 mg/mL | 70 mg/mL | 70 mg/mL |
特异性亚型抑制剂
Retinoid Receptor产品
| 产品目录 | 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.
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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。 |
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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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| 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。 |
||
| 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。 |
| 产品目录 | 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。 |
2018, 175(5):1244-1258 |
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。 |
2017, 8(16):26245-26255 2018, 40(8):702-708 |
|
| 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。 |
2017, 61(11). pii: e01368-17 2017, 25(4):620-624 |
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。 |
2013, 123(9):3941-51 |
|
| 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。 |
2017, 10.1074/jbc.M117.812537 |
|
| 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。 |
