1. GPCR/G Protein
  2. Cannabinoid Receptor

(±)-SLV319 (Synonyms: (±)-Ibipinabant; (±)-BMS6462)

Cat. No.: HY-14791A Purity: 99.49%
Handling Instructions

(±)-SLV319 is the racemate of SLV319. SLV319 is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.

For research use only. We do not sell to patients.
(±)-SLV319 Chemical Structure

(±)-SLV319 Chemical Structure

CAS No. : 362519-49-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
5 mg USD 108 In-stock
10 mg USD 192 In-stock
50 mg USD 792 In-stock
100 mg USD 1380 In-stock
200 mg   Get quote  
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

(±)-SLV319 is the racemate of SLV319. SLV319 is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM.

IC50 & Target

IC50: 22 nM (CB-1)[1]; Ki: 7.8 nM (CB-1)[2]

In Vitro

Cannabinoid receptor 1 (CB1R) antagonists appear to be promising drugs for the treatment of obesity, however, serious side effects have hampered their clinical application. 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].

In Vivo

Ibipinabant (3 mg/kg) reduces unfasted glucose to a significantly greater degree than rimonabant at the same dose on days 17, 28 and 38. Chronic treatment with ibipinabant significantly attenuates the progression of diabetes in ZDF rats, blunting the increase in blood glucose and HbA1c over time. Ibipinabant also reduces the hyperinsulinemia apparent at 6-8 weeks of age and attenuates the dramatic reduction in insulin levels observed 1-2 weeks later[3].

References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[3]

Rats: SLV319, rimonabant and rosiglitazone are suspended in a 10% dimethylacetamide, 10% cremophor, 10% ethanol and 70% water vehicle. Drugs are administered by oral gavage in a volume of 2 mL/kg body weight at 09:00 hours every day. Treatment groups are as follows: (i) Vehicle: ad libitum access to food (vehicle), (ii) Vehicle: restricted access to food (20% less than average food intake of ad libitum vehicle-treated group for the first 3 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) SLV319 (3 mg/kg) (IBI 3 mg/kg) and (vii) Ibipinabant (10 mg/kg) (IBI 10 mg/kg). Rosiglitazone is used as a positive control for its ability to delay β-cell decline, and rimonabant is used as a positive control for CB1 antagonism[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

487.4

Formula

C₂₃H₂₀Cl₂N₄O₂S

CAS No.

362519-49-1

SMILES

C/N=C(N1N=C(C2=CC=C(Cl)C=C2)C(C3=CC=CC=C3)C1)\NS(=O)(C4=CC=C(Cl)C=C4)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 31 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
(±)-SLV319
Cat. No.:
HY-14791A
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