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RTI-13951-33 hydrochloride

Catalog No. T12778 CAS T12778

Synonyms: RTI-13951-33 hydrochloride (2244884-08-8 free base)

RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist. RTI-13951-33 hydrochloride exhibited an EC 50 of 25 nM in vitro cAMP functional assay. RTI-13951-33 hydrochloride significantly reduces alcohol reinforcement and intake behaviors in rats [1].

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RTI-13951-33 hydrochloride Chemical Structure

RTI-13951-33 hydrochloride, CAS T12778

Pack Size	Availability	Price/USD	Quantity
25 mg	10-14 weeks	$ 1,360.00
50 mg	10-14 weeks	$ 2,280.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist. RTI-13951-33 hydrochloride exhibited an EC 50 of 25 nM in vitro cAMP functional assay. RTI-13951-33 hydrochloride significantly reduces alcohol reinforcement and intake behaviors in rats [1].
Targets&IC50	GPR88:（EC50）25 nM
In vitro	RTI-13951-33 is a potent and selective GPR88 agonist that effectively crosses the blood-brain barrier, demonstrating a significant effect with an EC50 value of 25 nM in GPR88 cAMP functional assays. It also increases [35S]-GTPγS binding in the mouse striatum with an EC50 of 535 nM, a response absent in GPR88 knockout (KO) mice. Despite its primary activity, RTI-13951-33 exhibits weak affinities for the kappa opioid receptor (KOR; Ki, 2.29 μM), the vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and a moderate affinity for the serotonin transporter (SERT; Ki, 0.75 μM). However, it demonstrates poor inhibition of SERT, with an IC50 of 25.1±2.7 μM.
In vivo	RTI-13951-33 (10 and 20 mg/kg, i.p.) decreases alcohol lever responses in a rat model of alcohol self-administration in a dose-dependent manner [1]. RTI-13951-33 (10 mg/kg, i.p.) shows sufficient brain penetration, with t 1/2 of 48 min and 87 min in rat plasma and brain [1].

Synonyms	RTI-13951-33 hydrochloride (2244884-08-8 free base)
Molecular Weight	532.5
Formula	C28H35Cl2N3O3
CAS No.	T12778

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (234.74 mM), Sonication is recommended.

References and Literature

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.

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Keywords

RTI-13951-33 hydrochloride T12778 Others 2244884-08-8 free base RTI-13951-33 hydrochloride (2244884-08-8 free base) RTI 13951 33 hydrochloride 2244884-08-8 RTI1395133 hydrochloride RTI-13951-33 Hydrochloride inhibitor inhibit

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