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RTI-13951-33

Catalog No. T12778L CAS 2244884-08-8

RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).

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RTI-13951-33, CAS 2244884-08-8

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,820.00
50 mg	8-10 weeks	$ 2,380.00
100 mg	8-10 weeks	$ 3,100.00

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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.

Biological Description

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Description	RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
Targets&IC50	GPR88:(EC50)25 nM
In vitro	RTI-13951-33 poorly inhibits SERT (IC50: 25.1 ± 2.7 μM). RTI-13951-33 elevates [35S]-GTPγS binding (EC50: 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice. RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; Ki, 2.29 μM), vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and moderate affinity at serotonin transporter (SERT; Ki, 0.75 μM) [1].
In vivo	RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently reduces alcohol lever responses in a rat model of alcohol self-administration. RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t1/2 of 48 min and 87 min in rat plasma and brain [1].

Molecular Weight	459.58
Formula	C28H33N3O3
CAS No.	2244884-08-8

Storage

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

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 2244884-08-8 Endocrinology/Hormones GPCR/G Protein GPR RTI1395133 RTI 13951 33 inhibitor inhibit

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