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Chemical Structure : LEO 134310
Catalog No.: 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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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.
| M.Wt | 604.700 | |
| Formula | C34H40N2O8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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