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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

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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 G蛋白偶联受体内分泌与激素 GPR RTI1395133 RTI 13951 33 Inhibitor inhibitor inhibit

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