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ARN 11391 is a selective enhancer of inositol triphosphate receptor type 1 (ITPR1). ARN 11391 can be used in the study of spinocerebellar ataxia[1]. | [Biological Activity]
Selective inositol triphosphate receptor type 1 (ITPR1) potentiator for wild-type as well as two ITPR1 SCA29 mutantsR269W or T267M.
ARN11391 is a selective inositol triphosphate receptor type 1 (ITPR1)but not ITPR2 or ITPR3potentiator (open channel probability (Po) = 0.2 with 20 μM ARN11391 and <0.01 without by on-nucleus nuclear patch-clamp using TPR1-YFP-expressing HEK293 cells) th at potenitates IP3- (by photolysis of caged IP3) and UPT-induced calcium increase in HEK293 transfectants expressing wild-type as well as ITPR1 SCA29 mutantsR269W or T267M (5 μM UTP with or without 10 μM ARN11391). | [References]
[1] Genovese M, et al. Pharmacological potentiators of the calcium signaling cascade identified by high-throughput screening. PNAS Nexus. 2022 Dec 9;2(1):pgac288. DOI:10.1093/pnasnexus/pgac288 |
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