|4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸|CsnPharm

CAS No.: 102121-60-8

4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)benzoic acid Catalog No. CSN12870

Synonyms: CD336;NSC608001;Ro 40-6055

AM580 is the stable retinobenzoic derivative that acts as an agonist of RARα.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述AM580 is a retinoic acid analog, working as a selective RARα agonist with EC50 values of 0.3, 8.6 and 13 nM for RARα, RARβ and RARγ respectively. AM580 at concentration of 100nM could recapitulate all of the T cell activation and type 2 cytokine-inducing effects of ATRA and 9-cis-RA on promotion of IL-4, IL-5 and IL-13 synthesis, while decreasing IFN-γ and TNF-α expression by activated human T cells and reduces the synthesis of IL-12p70 from accessory cells. Enhancing RA signaling by AM580 at concentration of 10nM profoundly promoted reprogramming of MEFs with transfected with four transcription factors (Oct4, Sox2, c-Myc, and Klf4), shown as substantial increase of the number of AP⁺ iPSC colonies.

动物研究

剂量

Mice: 3.75 mg/kg^[3] (i.p.), 2 mg/kg - 10 mg/kg^[4] (i.p.), 12.5 mg/kg (i.p.); 0.3 mg/kg^[1] (p.o., in diet), 0.6 mg/kg - 0.8 mg/kg^[5] (p.o., in drinking water)

给药途径

i.p., p.o.

动物药代数据

Animal	Rats^[4]
Dose	10 mg/kg
Administration	i.p.
V_d	1.5 ± 0.7 L/kg
T_1/2	1.7 ± 0.3 h
T_max	0.6 ± 0.4 h
CL	9.7 ± 3.2 ml/min/kg
C_max	5.8 ± 2.1 μg/ml
AUC	18.4 ± 5.4 μg·h/ml

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8454 mL
- 14.2272 mL
- 28.4545 mL
- 5 mM
- 0.5691 mL
- 2.8454 mL
- 5.6909 mL
- 10 mM
- 0.2845 mL
- 1.4227 mL
- 2.8454 mL

技术信息

CAS号

102121-60-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H25NO3

运输

蓝冰

分子量

351.44

别名

CD336;NSC608001;Ro 40-6055

溶解度

DMSO	70.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	24.0 mg/mL (68.3 mM)

动物实验配方

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4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)benzoic acid Catalog No. CSN12870

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