Name | Risdiplam |
Description | Risdiplam (RG7916) is a centrally and peripherally distributed and orally administrable small molecule SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels. |
In vitro | METHODS: LLC-PK1, MDCKII, L-MDR1 (LLC-PK1 cells transfected with human MDR1), L-Mdr1a (LLC-PK1 cells transfected with rodent Mdr1a), M-BCRP (MDCKII cells transfected with human breast cancer resistance protein; BCRP), and M-Bcrp1 (MDCKII cells transfected with rodent Bcrp1) cells were treated with Risdiplam (RG7916) (1 μM) and 10 μM Lucifer Yellow added to the donor compartment to initiate transcellular transport.
RESULTS Risdiplam had a mean passive permeability of approximately 350 nm/s in parental LLC-PK1 cells. Similar permeability was observed in L-MDR1, L-Mdra1, M-BCRP, and M-Bcrp cells in the presence of the inhibitor. [1] |
In vivo | METHODS: Wistar rats received either a single oral dose of 14C-risdiplam (RO7034067) (by gastric gavage) or a single intravenous dose of 14C-risdiplam (by tail vein injection). Dose levels for oral and intravenous doses were 5 or 2 mg/kg, respectively.
RESULTS Radioactive 14C-risdiplam (RO7034067) was rapidly and extensively distributed in rat QWBA after oral administration, with peak concentrations in most tissues measured at 2 hours. Radioactivity concentrations in plasma and tissues declined during the study period. [1] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : < 1 mg/mL (insoluble), Sonication is recommended. Ethanol : 2 mg/mL (4.98 mM), Sonication is recommended. H2O : 2.22 mg/mL (5.53 mM), when pH is adjusted to 6 with HCl. Sonication is recommended.
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Keywords | RG 7916 | Inhibitor | RO 7034067 | DNA/RNA Synthesis | RG-7916 | RO-7034067 | Risdiplam | inhibit |
Inhibitors Related | Rifampicin | 5-Fluorouracil | Ribavirin | Guanidine hydrochloride | 2,4-D | Resveratrol | Trimethoprim | Azelaic acid | Acyclovir | Thymidine | Temozolomide | Folic acid |
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