RTI-13951-33


Catalog No. Size PriceQuantity
M33297-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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.

Product information

CAS Number: 2244884-08-8

Molecular Weight: 459.58

Formula: C28H33N3O3

Chemical Name: (1R,2R)-N-[(2R,3R)-2-amino-3-methoxybutyl]-N-[4'-(methoxymethyl)-[1,1'-biphenyl]-4-yl]-2-(pyridin-2-yl)cyclopropane-1-carboxamide

Smiles: C[C@@H](OC)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1C1=CC=CC=N1)C1C=CC(=CC=1)C1C=CC(COC)=CC=1

InChiKey: XCHHIKJEGXHKLQ-UJTWYAIMSA-N

InChi: InChI=1S/C28H33N3O3/c1-19(34-3)26(29)17-31(28(32)25-16-24(25)27-6-4-5-15-30-27)23-13-11-22(12-14-23)21-9-7-20(8-10-21)18-33-2/h4-15,19,24-26H,16-18,29H2,1-3H3/t19-,24-,25-,26-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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), however, RTI-13951-33 poorly inhibits SERT (IC50, 25.1 ± 2.7 μM).

In Vivo:

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. RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration.

Products are for research use only. Not for human use.

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