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RTI-13951-33 hydrochloride 

Cat. No.: HY-112612A Purity: 99.52%
Handling Instructions

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

For research use only. We do not sell to patients.

RTI-13951-33 hydrochloride Chemical Structure

RTI-13951-33 hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 644 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats[1].

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; 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)[1].

In Vivo

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].
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

532.50

Formula

C₂₈H₃₅Cl₂N₃O₃

SMILES

COCC1=CC=C(C2=CC=C(N(C[[email protected]@H](N)[[email protected]@H](C)OC)C([[email protected]]3[[email protected]](C4=CC=CC=N4)C3)=O)C=C2)C=C1.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (234.74 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8779 mL 9.3897 mL 18.7793 mL
5 mM 0.3756 mL 1.8779 mL 3.7559 mL
10 mM 0.1878 mL 0.9390 mL 1.8779 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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KeyWords:

RTI-13951-33 | Others | Inhibitor | inhibitor | inhibit

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Product name:
RTI-13951-33 hydrochloride
Cat. No.:
HY-112612A
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