| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
RTI-122 dihydrochloride effectively activated human GPR88 in CHO cells stably expressing PPLS-HA-GPR88, with an EC50 value of 10.8 nM for cAMP at 30 min; it also effectively activated the G protein signaling pathway of human GPR88 in the cell membrane of PPLS-HA-hGPR88-CHO cells, with an EC50 value of 11.5 nM for [35S]GTPγS at 60 min [1]. RTI-122 dihydrochloride (30 μM; 60 min) had no activity in the striatal membrane of GPR88 knockout mice, but it selectively activated endogenous mouse GPR88 in the striatal membrane of wild-type mice, with an EC50 value of 155 nM for [35S]GTPγS [1]. RTI-122 dihydrochloride showed good metabolic stability in mouse liver microsomes, with a half-life of 24.6 min and a clearance rate of 56.4 μL/min/mg [1]. RTI-122 dihydrochloride (10 μM; 90 min) has good blood-brain barrier penetration ability. In MDCK-MDR1 cell assay, its Papp value from the apex to the lateral base is 2.8 × 10⁻⁶ cm/s, and the efflux ratio is 2.5[1]. RTI-122 dihydrochloride (1 μM; 6 h) has a high binding rate of up to 99.5% to mouse plasma proteins[1].
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| ln Vivo |
RTI-122 (10 mg/kg; intraperitoneal injection; single dose) dihydrochloride significantly reduced binge drinking behavior in male C57BL/6J mice, with efficacy comparable to RTI-13951-33 at 30 mg/kg [1]. RTI-122 (10–20 mg/kg; intraperitoneal injection; single dose) dihydrochloride reduced spontaneous kinetic activity in male C57BL/6J mice in a dose-dependent manner. Both the 10 mg/kg and 20 mg/kg groups showed efficacy within 20 minutes of injection, while only the 20 mg/kg group showed efficacy within 20–40 minutes [2]. RTI-122 (10–20 mg/kg; intraperitoneal injection; single dose) dihydrochloride induced a specific reduction in alcohol intake in wild-type GPR88 mice. Both 10 mg/kg and 20 mg/kg doses were effective in male mice, while only the 20 mg/kg dose was effective in female mice [2]. RTI-122 (5–10 mg/kg; intraperitoneal injection; single dose) dihydrochloride dose-dependently reduced operant alcohol self-administration behavior in alcohol-loving male and female rats, but had no effect on sucrose self-administration, suggesting that it plays a regulatory role in alcohol-specific reward[2]. RTI-122 (2.5–10 mg/kg; intraperitoneal injection; single dose) dihydrochloride reduced the motivation of alcohol-loving male and female rats to self-administer pure alcohol and quinine-mixed alcohol[2]. RTI-122 (20 mg/kg; intraperitoneal injection; single dose) dihydrochloride reduced yohimbine-induced alcohol craving behavior in male and female alcohol-loving rats and inhibited relapse of alcohol self-administration in both sexes at doses of 10 mg/kg and 20 mg/kg[2].
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| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 8-9 weeks old) [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: Compared with the saline control group, it significantly reduced binge-drinking alcohol intake, with an effect comparable to that of the reference compound RTI-13951-33 at a dose of 30 mg/kg. It had no effect on water intake. Animal/Disease Models:C57BL/6J (male, 3-5 months old, 25-35 g) [2] Doses: 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: Spontaneous movement decreased in a dose-dependent manner within the first 20 minutes after injection, with the effects being particularly pronounced in the 10 mg/kg and 20 mg/kg dose groups. During the 20-40 minute period, a decrease in movement was observed only in the 20 mg/kg dose group. No effect on movement was observed during the 40-60 minute period. Animal/Disease Models:Alcohol-Addicted Mice (P) (Male and Female) [2] Doses: 2.5 mg/kg; 5 mg/kg; 10 mg/kg Route of Administration: Intraperitoneal injection; Single dose Experimental Results: Alcohol lever response was reduced, with the reduction being particularly significant at 5 mg/kg and 10 mg/kg doses. Alcohol intake was reduced, with the reduction being particularly significant at 5 mg/kg and 10 mg/kg doses. In the alcohol self-administration test, the 10 mg/kg dose group had a reduced movement frequency. There was no effect on sucrose lever response or sucrose intake. In the sucrose self-administration test, the 10 mg/kg dose group had a reduced movement frequency. In the seeking phase, the 20 mg/kg dose group had a reduced lever response. At both 10 mg/kg and 20 mg/kg doses, the lever response was reduced in the restart phase. During the search phase, the movement frequency decreased at both dosages. |
| References |
| Molecular Formula |
C29H36CL2FN3O3
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|---|---|
| Molecular Weight |
564.52
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| Related CAS # |
RTI-122
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| Appearance |
White to light yellow solid
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| SMILES |
CO[C@H](C)[C@H](N)CN(C1=CC=C(C2=CC=C(C=C2)OC(C)C)C=C1)C([C@H]3[C@H](C4=CC=C(C=N4)F)C3)=O.Cl.Cl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~177.14 mM; with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7714 mL | 8.8571 mL | 17.7142 mL | |
| 5 mM | 0.3543 mL | 1.7714 mL | 3.5428 mL | |
| 10 mM | 0.1771 mL | 0.8857 mL | 1.7714 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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