| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Ibipinabant (racemic), also known as (±)-SLV319; BMS-646256; JD-5001, is the racemic mixture of SLV319 and is a novel, potent and selective antagonist/inverse agonist of cannabinoid-1 (CB-1) receptor with an IC50 of 22 nM. SLV-319 (Ibipinibant) analogs were created with the goal of minimizing brain exposure while preserving the parent compound's receptor affinity and selectivity. One of these compounds' effects on liver weight and enzymes, insulin sensitivity, glucose tolerance, and plasma triglyceride levels lend credence to the theory that many of the advantageous metabolic effects of globally active CB(1) blockers can be produced by blocking peripheral CB(1) receptors alone. In light of this, PR CB(1) inverse agonists may offer a less risky option for treating metabolic disorders such as diabetes, liver disease, dyslipidemias, and obesity than highly brain-penetrant medications.
| Targets |
CB-1 ( IC50 = 22 nM )
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|---|---|
| ln Vitro |
Though their clinical application has been hindered by serious side effects, cannabinoid receptor 1 (CB1R) antagonists seem to be promising medications for the treatment of obesity. Ibipinabant is a new, potent [Ki (CB1)=7.8 nM] and selective [Ki (CB2)=7.943 nM] CB1 antagonist [pA2 for arachidonic acid release in CHO cells=9.9] with in vitro pharmacological characteristics similar to rimonabant including inverse agonism and brain penetrance[3].
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| ln Vivo |
On days 17, 28, and 38, (±)-Ibipinabant ((±)-SLV319) (3 mg/kg) significantly lowers unfasted glucose compared to rimonabant at the same dose. In ZDF rats, long-term administration of (±)-Ibipinabant ((±)-SLV319) substantially slows down the development of diabetes, reducing the rate of blood glucose and HbA1c increases over time. Additionally, if administered 6–8 weeks after birth, ibipinabant lessens the hyperinsulinemia that is visible and lessens the sharp decline in insulin levels that occurs 1-2 weeks later[3].
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| Animal Protocol |
Rats: SLV319, rimonabant, and rosiglitazone are suspended in a vehicle consisting of 70% water, 10% ethanol, 10% cremophor, and 10% dimethylacetamide. Oral gavage is used to administer drugs at 09:00 hours daily in a volume of 2 mL/kg body weight. These are the treatment groups: (i) Ad libitum access to food (vehicle); (ii) Restricted access to food (20% less than the average food intake of the ad libitum vehicle-treated group for the first three days of the study, then 10% less than the average food intake of the ad libitum vehicle-treated group for the remainder of the study) (restricted); (iii) Rosiglitazone (4 mg/kg); (iv) Rimonabant (3 mg/kg) (RIM 3 mg/kg); (v) Rimonabant (10 mg/kg) (RIM 10 mg/kg); (vi) (±)-Ibipinabant ((±)-SLV319) (3 mg/kg) (IBI 3 mg/kg); and (vii) Ibipinabant (10 mg/kg) (IBI 10 mg/kg). For its capacity to postpone β-cell decline, rosiglitazone is employed as a positive control, and rimonabant is employed as a positive control for CB1 antagonism[3].
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| References |
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| Molecular Formula |
C23H20CL2N4O2S
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|---|---|
| Molecular Weight |
487.4015
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| Exact Mass |
486.07
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| Elemental Analysis |
C, 56.68; H, 4.14; Cl, 14.55; N, 11.50; O, 6.57; S, 6.58
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| CAS # |
362519-49-1
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| Related CAS # |
Ibipinabant; 464213-10-3
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| Appearance |
Solid powder
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| SMILES |
CN=C(NS(=O)(=O)C1=CC=C(C=C1)Cl)N2CC(C(=N2)C3=CC=C(C=C3)Cl)C4=CC=CC=C4
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| InChi Key |
AXJQVVLKUYCICH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20Cl2N4O2S/c1-26-23(28-32(30,31)20-13-11-19(25)12-14-20)29-15-21(16-5-3-2-4-6-16)22(27-29)17-7-9-18(24)10-8-17/h2-14,21H,15H2,1H3,(H,26,28)
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| Chemical Name |
5-(4-chlorophenyl)-N-(4-chlorophenyl)sulfonyl-N'-methyl-4-phenyl-3,4-dihydropyrazole-2-carboximidamide
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| Synonyms |
JD5001; JD-5001; JD 5001; (±)-SLV-319; (±)-SLV 319; SLV319; (±)-BMS-646256; (±)-BMS646256; (±)-BMS 646256; (±)-Ibipinabant
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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) |
DMSO: ≥ 31 mg/mL (~63.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0517 mL | 10.2585 mL | 20.5170 mL | |
| 5 mM | 0.4103 mL | 2.0517 mL | 4.1034 mL | |
| 10 mM | 0.2052 mL | 1.0259 mL | 2.0517 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00541567 | Completed | Drug: ibipinabant | Obesity and Type 2 Diabetes | Solvay Pharmaceuticals | March 2008 | Phase 2 Phase 3 |
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