RTI-13951-33hydrochloride
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 532.50 |
| Molecular Formula | C28H35Cl2N3O3 |
| SMILES | COCC1=CC=C(C2=CC=C(N(C[C@@H](N)[C@@H](C)OC)C([C@H]3[C@H](C4=CC=CC=N4)C3)=O)C=C2)C=C1.Cl.Cl |
1 Publications Citing Use of MCE
Summary
IC50 & Target
EC50: 25 nM (GPR88) [1]
In Vitro
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC
50
of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [
35
S]-GTPγS binding (EC
50
, 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; K
i
, 2.29 μM), vesicular monoamine transporter (VMAT; K
i
, 4.23 μM), and moderate affinity at serotonin transporter (SERT; K
i
, 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC
50
, 25.1±2.7 μM)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 t
1/2
of 48 min and 87 min in rat plasma and brain
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 93.90 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 93.90 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (187.79 mM); Clear solution; Need ultrasonic
-
2.
-
3.
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
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution