| Bioactivity | ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM)[1]. ML 145 has no significant activity for GPR35 at either rodent ortholog[2]. | ||||||||||||
| Target | IC50/EC50: 20.1 nM (GPR35), 21.7 μM (GPR55) | ||||||||||||
| Invitro | ML 145 (10 μM) also fully blocks internalization of human FLAG-GPR35-eYFP in response to varying concentrations of Zaprinast, Cromolyn disodium, and Pamoate[2]. ML 145 is either without effect (mouse) or displays only a small and apparently noncompetitive inhibitory effect (rat) at the rodent orthologs[2]. ML 145 acts as a competitive antagonist for a number of agonists at human GPR35 and has an IC50 value against EC80 concentrations of various GPR35 agonists in the region of 20 nM[1]. | ||||||||||||
| Name | ML 145 | ||||||||||||
| CAS | 1164500-72-4 | ||||||||||||
| Formula | C24H22N2O5S2 | ||||||||||||
| Molar Mass | 482.57 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Heynen-Genel S, et al. Selective GPR35 Antagonists - Probes 1 & 2. National Center for Biotechnology Information (US); 2010-2010 Feb 28. [2]. Laura Jenkins, et al. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther. 2012 Dec;343(3):683-95. |
ML 145
CAS: 1164500-72-4 F: C24H22N2O5S2 W: 482.57
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fo
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