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Cat. No.: HY-112612

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RTI-13951-33

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC₅₀ of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats.

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CAS No.: 2244884-08-8
Formule: C₂₈H₃₃N₃O₃
Masse moléculaire:459.58

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

RTI-13951-33 Chemical Structure

CAS No.: 2244884-08-8

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Description

IC₅₀ & Target

EC50: 25 nM (GPR88)^[1]

In Vitro

RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC₅₀ of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [³⁵S]-GTPγS binding (EC₅₀， 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice^[1].
RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; K_i, 2.29 μM), vesicular monoamine transporter (VMAT; K_i, 4.23 μM), and moderate affinity at serotonin transporter (SERT; K_i, 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC₅₀, 25.1 ± 2.7 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t_1/2 of 48 min and 87 min in rat plasma and brain^[1].
RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2244884-08-8
Masse moléculaire 459.58
Formule C₂₈H₃₃N₃O₃
SMILES

COCC1=CC=C(C2=CC=C(N(C[C@@H](N)[C@@H](C)OC)C([C@H]3[C@H](C4=CC=CC=N4)C3)=O)C=C2)C=C1
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Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

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bioRxiv

Persistent changes in nociceptor translatomes govern hyperalgesic priming in mouse models. [Abstract]

2024 Aug 8:2024.08.07.606891. PMID: 39149295
bioRxiv

2020 May.

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Jin C, et al. Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake. J Med Chem. 2018 Aug 9;61(15):6748-6758. [Content Brief]

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RTI-13951-33

2 Cited Publications

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RTI-13951-33

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