HY-109153 Search Results


paltusotine  (MedChemExpress)
89
MedChemExpress paltusotine
Paltusotine, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 89/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/paltusotine/product/MedChemExpress
Average 89 stars, based on 1 article reviews
paltusotine - by Bioz Stars, 2026-02
89/100 stars
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ralmitaront  (MedChemExpress)
94
MedChemExpress ralmitaront
Functional evaluation of <t>ralmitaront</t> at trace amine-associated receptor-1 (TAAR1). (A) Chemical structures of the TAAR1 agonists ulotaront and ralmitaront. (B) Comparison of the recruitment of LgBiT-miniGα s to 3xHA-9β2-TAAR1-SmBiT by p-tyramine, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. Data shown are from 15 minutes after agonist addition. (C) Time dependence of pEC 50 s in the TAAR1 NanoBiT assay. (D) Stimulation of cAMP production measured as light intensity change in HEK293T cells expressing 3xHA-9β2-TAAR1 and GloSensor 22F at different time points following agonist addition. Each data point represents mean ± SEM from 3 separate experiments, each using 8 replicate wells for each agonist concentration. (E) Time dependence of pEC 50 s in the TAAR1 cAMP assay. (F) Activation of G protein–coupled inward-rectifying potassium channels upon ulotaront and ralmitaront application to Xenopus oocytes expressing G protein-coupled inward rectifier potassium (GIRK) 1/4 channels, 3xHA-9β2-TAAR1, and G s . Current amplitudes at 1 minute following application of each agonist concentration were normalized, within cells, to the response to 100 µM p-tyramine. Each data point represents mean ± SEM from 4 to 8 separate oocytes. (G) Activation rates of TAAR1-mediated GIRK responses elicited by ralmitaront (slope 0.006 ± 0.001 s −1 µM −1 ; y-intercept 0.019 ± 0.007 s −1 , n = 3–7 oocytes, concentrations tested: 1 µM, 3 µM, 6.5 µM, 10 µM) and ulotaront (slope 0.163 ± 0.022 s −1 µM −1 ; y-intercept 0.035 ± 0.008 s −1 , n = 3–6 oocytes, concentrations tested: 100 nM, 300 nM, 650 nM). (H) Response decay time courses following washout of 3 µM ralmitaront (n = 4) or 300 nM of ulotaront (n = 5). The TAAR1 agonists were applied for 15 seconds, and the washout duration was 260 seconds. Data are presented as mean ± SEM.
Ralmitaront, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/ralmitaront/product/MedChemExpress
Average 94 stars, based on 1 article reviews
ralmitaront - by Bioz Stars, 2026-02
94/100 stars
  Buy from Supplier

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Functional evaluation of ralmitaront at trace amine-associated receptor-1 (TAAR1). (A) Chemical structures of the TAAR1 agonists ulotaront and ralmitaront. (B) Comparison of the recruitment of LgBiT-miniGα s to 3xHA-9β2-TAAR1-SmBiT by p-tyramine, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. Data shown are from 15 minutes after agonist addition. (C) Time dependence of pEC 50 s in the TAAR1 NanoBiT assay. (D) Stimulation of cAMP production measured as light intensity change in HEK293T cells expressing 3xHA-9β2-TAAR1 and GloSensor 22F at different time points following agonist addition. Each data point represents mean ± SEM from 3 separate experiments, each using 8 replicate wells for each agonist concentration. (E) Time dependence of pEC 50 s in the TAAR1 cAMP assay. (F) Activation of G protein–coupled inward-rectifying potassium channels upon ulotaront and ralmitaront application to Xenopus oocytes expressing G protein-coupled inward rectifier potassium (GIRK) 1/4 channels, 3xHA-9β2-TAAR1, and G s . Current amplitudes at 1 minute following application of each agonist concentration were normalized, within cells, to the response to 100 µM p-tyramine. Each data point represents mean ± SEM from 4 to 8 separate oocytes. (G) Activation rates of TAAR1-mediated GIRK responses elicited by ralmitaront (slope 0.006 ± 0.001 s −1 µM −1 ; y-intercept 0.019 ± 0.007 s −1 , n = 3–7 oocytes, concentrations tested: 1 µM, 3 µM, 6.5 µM, 10 µM) and ulotaront (slope 0.163 ± 0.022 s −1 µM −1 ; y-intercept 0.035 ± 0.008 s −1 , n = 3–6 oocytes, concentrations tested: 100 nM, 300 nM, 650 nM). (H) Response decay time courses following washout of 3 µM ralmitaront (n = 4) or 300 nM of ulotaront (n = 5). The TAAR1 agonists were applied for 15 seconds, and the washout duration was 260 seconds. Data are presented as mean ± SEM.

Journal: International Journal of Neuropsychopharmacology

Article Title: In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics

doi: 10.1093/ijnp/pyad049

Figure Lengend Snippet: Functional evaluation of ralmitaront at trace amine-associated receptor-1 (TAAR1). (A) Chemical structures of the TAAR1 agonists ulotaront and ralmitaront. (B) Comparison of the recruitment of LgBiT-miniGα s to 3xHA-9β2-TAAR1-SmBiT by p-tyramine, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. Data shown are from 15 minutes after agonist addition. (C) Time dependence of pEC 50 s in the TAAR1 NanoBiT assay. (D) Stimulation of cAMP production measured as light intensity change in HEK293T cells expressing 3xHA-9β2-TAAR1 and GloSensor 22F at different time points following agonist addition. Each data point represents mean ± SEM from 3 separate experiments, each using 8 replicate wells for each agonist concentration. (E) Time dependence of pEC 50 s in the TAAR1 cAMP assay. (F) Activation of G protein–coupled inward-rectifying potassium channels upon ulotaront and ralmitaront application to Xenopus oocytes expressing G protein-coupled inward rectifier potassium (GIRK) 1/4 channels, 3xHA-9β2-TAAR1, and G s . Current amplitudes at 1 minute following application of each agonist concentration were normalized, within cells, to the response to 100 µM p-tyramine. Each data point represents mean ± SEM from 4 to 8 separate oocytes. (G) Activation rates of TAAR1-mediated GIRK responses elicited by ralmitaront (slope 0.006 ± 0.001 s −1 µM −1 ; y-intercept 0.019 ± 0.007 s −1 , n = 3–7 oocytes, concentrations tested: 1 µM, 3 µM, 6.5 µM, 10 µM) and ulotaront (slope 0.163 ± 0.022 s −1 µM −1 ; y-intercept 0.035 ± 0.008 s −1 , n = 3–6 oocytes, concentrations tested: 100 nM, 300 nM, 650 nM). (H) Response decay time courses following washout of 3 µM ralmitaront (n = 4) or 300 nM of ulotaront (n = 5). The TAAR1 agonists were applied for 15 seconds, and the washout duration was 260 seconds. Data are presented as mean ± SEM.

Article Snippet: In vitro transcription was performed using the T7 mMessage mMachine kit (Ambion, Austin, TX, USA). cRNA concentration and purity were assessed by spectrophotometry. p-Tyramine, dopamine, quinpirole, and 5-HT were from Sigma-Aldrich (St. Louis, MO, USA), and ulotaront, ralmitaront, and RTI-7470-44 were from MedChemExpress (Monmouth Junction, NJ, USA).

Techniques: Functional Assay, Comparison, Concentration Assay, Expressing, cAMP Assay, Activation Assay

Ralmitaront lacks detectable activity at the serotonin 5-HT 1A receptor (5-HT 1A R) and the dopamine D 2 receptor (D 2 R). (A) Comparison of the recruitment of LgBiT-miniGα i to 5-HT 1A R-SmBiT by 5-HT, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. (B) Inhibition of cAMP production, measured as light intensity change, in HEK293T cells expressing the 5-HT 1A R and GloSensor 22F at 40 minutes following agonist addition. Each data point represents mean ± SEM from 3 separate experiments, each using 8 replicate wells for each agonist concentration. (C) Average traces representing mean ± SEM showing responses to application of 30 µM ulotaront (n = 5), 30 µM ralmitaront (n = 6), and 100 nM 5-HT (n = 11) in Xenopus oocytes coexpressing the 5-HT 1A R with G protein-coupled inward rectifier potassium (GIRK) 1/4 channels. (D) Comparison of the recruitment of LgBiT-miniGα i to D 2 R-SmBiT by quinpirole, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. (E) Inhibition of cAMP production, measured as light intensity change, in HEK293T cells expressing the D 2 R and GloSensor 22F at 40 minutes following agonist addition. Each data point represents mean ± SEM of data from 3 independent experiments, each using 8 replicate wells for each agonist concentration. (F) Average traces representing mean ± SEM showing responses to applications of 30 µM ulotaront (n = 4), 30 µM ralmitaront (n = 6), and 1 µM dopamine (n = 10), respectively, to Xenopus oocytes co-expressing the D 2 R with GIRK1/4 channels.

Journal: International Journal of Neuropsychopharmacology

Article Title: In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics

doi: 10.1093/ijnp/pyad049

Figure Lengend Snippet: Ralmitaront lacks detectable activity at the serotonin 5-HT 1A receptor (5-HT 1A R) and the dopamine D 2 receptor (D 2 R). (A) Comparison of the recruitment of LgBiT-miniGα i to 5-HT 1A R-SmBiT by 5-HT, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. (B) Inhibition of cAMP production, measured as light intensity change, in HEK293T cells expressing the 5-HT 1A R and GloSensor 22F at 40 minutes following agonist addition. Each data point represents mean ± SEM from 3 separate experiments, each using 8 replicate wells for each agonist concentration. (C) Average traces representing mean ± SEM showing responses to application of 30 µM ulotaront (n = 5), 30 µM ralmitaront (n = 6), and 100 nM 5-HT (n = 11) in Xenopus oocytes coexpressing the 5-HT 1A R with G protein-coupled inward rectifier potassium (GIRK) 1/4 channels. (D) Comparison of the recruitment of LgBiT-miniGα i to D 2 R-SmBiT by quinpirole, ulotaront, and ralmitaront in the NanoBiT assay. Each data point represents mean ± SEM from 3 separate experiments, each using 2 replicate wells for each agonist concentration. (E) Inhibition of cAMP production, measured as light intensity change, in HEK293T cells expressing the D 2 R and GloSensor 22F at 40 minutes following agonist addition. Each data point represents mean ± SEM of data from 3 independent experiments, each using 8 replicate wells for each agonist concentration. (F) Average traces representing mean ± SEM showing responses to applications of 30 µM ulotaront (n = 4), 30 µM ralmitaront (n = 6), and 1 µM dopamine (n = 10), respectively, to Xenopus oocytes co-expressing the D 2 R with GIRK1/4 channels.

Article Snippet: In vitro transcription was performed using the T7 mMessage mMachine kit (Ambion, Austin, TX, USA). cRNA concentration and purity were assessed by spectrophotometry. p-Tyramine, dopamine, quinpirole, and 5-HT were from Sigma-Aldrich (St. Louis, MO, USA), and ulotaront, ralmitaront, and RTI-7470-44 were from MedChemExpress (Monmouth Junction, NJ, USA).

Techniques: Activity Assay, Comparison, Concentration Assay, Inhibition, Expressing