LEO 134310 | GR agonist | Probechem Biochemicals

Chemical Structure : LEO 134310

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LEO 134310 (LP 0155)

货号: PC-73325Not For Human Use, Lab Use Only.

LEO 134310 (LP 0155) is a non-steroidal, potent and selective glucocorticoid receptor (GR) agonist (EC50=2 nM, hPBMC).

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生物&药学活性

LEO 134310 (LP 0155) is a non-steroidal, potent and selective glucocorticoid receptor (GR) agonist (EC50=2 nM, hPBMC).
LEO 134310 is rapidly deactivated in the blood resulting in low systemic exposure and a higher therapeutic index in the TPA-induced skin inflammation mouse model compared with betamethasone valerate (BMV) and clobetasol propionate (CP).
LEO 134310 displays high selectivity for GR in a panel of nuclear receptors, including the mineralocorticoid receptor (MR).
LEO 134310 exhibits full efficacy on GR transactivation and transrepression.
LEO 134310 may be suitable for long-term topical treatment of inflammatory skin diseases.

物理化学性质&存储条件

分子量	604.700
分子式	C34H40N2O8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-1-((R)-5-oxotetrahydrofuran-3-carbonyl)piperidin-3-yl 4-((1R,2S)-1-(4-cyclopropylphenyl)-2-((R)-tetrahydrofuran-2-carboxamido)propoxy)benzoate

参考文献

1. Eirefelt S, et al. Sci Rep. 2022 Jan 27;12(1):1501.

2. Dack KN, et al. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127402.

LEO 134310 (LP 0155)

生物&药学活性

物理化学性质&存储条件

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LEO 134310 (LP 0155)

生物&药学活性

物理化学性质&存储条件

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